NAMPT and ROCK inhibitors

ABSTRACT

Disclosed are isoindoline carboxamide, dihydropyrrolopyridine carboxamide, and dihydropyrrolopyrimidine carboxamide compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are isoindoline carboxamide, dihydropyrrolopyridine carboxamide, and dihydropyrrolopyrimidine carboxamide compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.

RELATED APPLICATION INFORMATION

This application is a continuation of U.S. application Ser. No. 13/294,303, filed Nov. 11, 2011, which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/413,722, filed Nov. 15, 2010, U.S. Provisional Application Ser. No. 61/474,015, filed Apr. 11, 2011, and U.S. Provisional Application Ser. No. 61/525,405, filed Aug. 19, 2011, the contents of which are incorporated by reference in their entirety.

FIELD OF THE INVENTION

This invention pertains to compounds which inhibit the activity of NAMPT, compositions containing the compounds, and methods of treating diseases during which NAMPT is expressed. This invention also pertains to compounds which inhibit the activity of ROCK, compositions containing the compounds, and methods of treating diseases during which ROCK is expressed.

BACKGROUND OF THE INVENTION

NAD+ (nicotinamide adenine dinucleotide) is a coenzyme that plays a critical role in many physiologically essential processes (Ziegkel, M. Eur. J. Biochem. 267, 1550-1564, 2000). NAD is necessary for several signaling pathways including among others poly ADP-ribosylation in DNA repair, mono-ADP-ribosylation in both the immune system and G-protein-coupled signaling, and NAD is also required by sirtuins for their deacetylase activity (Garten, A. et al Trends in Endocrinology and Metabolism, 20, 130-138, 2008).

NAMPT (also known as pre-B-cell-colony-enhancing factor (PBEF) and visfatin) is an enzyme that catalyzes the phosphoribosylation of nicotinamide and is the rate-limiting enzyme in one of two pathways that salvage NAD.

Increasing evidence suggests that NAMPT inhibitors have potential as anticancer agents. Cancer cells have a higher basal turnover of NAD and also display higher energy requirements compared with normal cells. Additionally, increased NAMPT expression has been reported in colorectal cancer (Van Beijnum, J. R. et al Int. J. Cancer 101, 118-127, 2002) and NAMPT is involved in angiogenesis (Kim, S. R. et al. Biochem. Biophys. Res. Commun. 357, 150-156, 2007). Small-molecule inhibitors of NAMPT have been shown to cause depletion of intracellular NAD+ levels and ultimately induce tumor cell death (Hansen, C M et al. Anticancer Res. 20, 42111-4220, 2000) as well as inhibit tumor growth in xenograft models (Olese, U. H. et al. Mol Cancer Ther. 9, 1609-1617, 2010).

NAMPT inhibitors also have potential as therapeutic agents in inflammatory and metabolic disorders (Galli, M. et al Cancer Res. 70, 8-11, 2010). For example, NAMPT is the predominant enzyme in T and B lymphocytes. Selective inhibition of NAMPT leads to NAD+ depletion in lymphocytes blocking the expansion that accompanies autoimmune disease progression whereas cell types expressing the other NAD+ generating pathways might be spared. A small molecule NAMPT inhibitor (FK866) has been shown to selectively block proliferation and induce apoptosis of activated T cells and was efficacious in animal models of arthritis (collagen induced arthritis) (Busso, N. et al. Plos One 3, e2267, 2008). FK866 ameliorated the manifestations of experimental autoimmune encephalomyelitis (EAE), a model of T-cell mediated autoimmune disorders. (Bruzzone, S et al. Plos One 4, e7897, 2009). NaMPT activity increases NF-kB transcriptional activity in human vascular endothelial cell, resulting in MMP-2 and MMP-9 activation, suggesting a role for NAMPT inhibitors in the prevention of inflammatory mediated complications of obesity and type 2 diabetes (Adya, R. et. Al. Diabetes Care, 31, 758-760, 2008).

Rho kinases (ROCKs), the first Rho effectors to be described, are serine/threonine kinases that are important in fundamental processes of cell migration, cell proliferation and cell survival. Abnormal activation of the Rho/ROCK pathway has been observed in various disorders. Examples of disease states in which compounds with ROCK inhibition have potentially beneficial therapeutic effects due to their anti vasospasm activity includes cardiovascular diseases such as hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension and atherosclerosis. This muscle relaxing property is also beneficial for treating asthma, male erectile dysfunctions, female sexual dysfunction, and over-active bladder syndrome. Injury to the adult vertebrate brain and spinal cord activates ROCKs, thereby inhibiting neurite growth and sprouting. Inhibition of ROCKs results in induction of new axonal growth, axonal rewiring across lesions within the CNS, accelerated regeneration and enhanced functional recovery after acute neuronal injury in mammals (spinal-cord injury, traumatic brain injury). Inhibition of the Rho/ROCK pathway has also proved to be efficacious in other animal models of neurodegeneration like stroke, inflammatory and demyelinating diseases, Alzheimer's disease as well as for the treatment of pain. Rho/ROCK pathway inhibitors therefore have potential for preventing neurodegeneration and stimulating neuroregeneration in various neurological disorders, including spinal-cord injury, Alzheimer's disease, stroke, multiple sclerosis, amyotrophic lateral sclerosis, as well as for the treatment of pain. ROCK inhibitors have been shown to possess anti-inflammatory properties. Thus, compounds of the invention can be used as treatment for neuroinflammatory diseases such as stroke, multiple sclerosis, Alzheimer's disease, Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, and inflammatory pain, as well as other diseases such as rheumatoid arthritis, osteoarthritis, asthma, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, Lupus, and inflammatory bowel disease. Since ROCK inhibitors reduce cell proliferation and cell migration, they could be useful in treating cancer and tumor metastasis. Further more, there is evidence suggesting that ROCK inhibitors suppress cytoskeletal rearrangement upon virus invasion, thus they also have potential therapeutic value in anti-viral and anti-bacterial applications. ROCK inhibitors are also useful for the treatment of insulin resistance and diabetes. Further, ROCK inhibitors have been shown to ameliorate progression of cystic fibrosis (Abstract S02.3, 8th World Congress on Inflammation, Copenhagen, Denmark, Jun. 16-20, 2007).

In addition, Rho-associated coiled-coil forming protein kinases (ROCK)-1 and -2, have been shown to enhance myosin light chain (MLC) phosphorylation by inhibiting MLC phosphatase as well as phosphorylating MLC. This results in the regulation of actin-myosin contraction. Recent reports have demonstrated that inhibition of ROCK results in disruption of inflammatory cell chemotaxis as well as inhibition of smooth muscle contraction in models of pulmonary inflammation associated with asthma. Therefore, the inhibitors of the Rho/ROCK pathway may be useful for the treatment of asthma.

SUMMARY OF THE INVENTION

One embodiment of this invention, therefore, pertains to compounds and pharmaceutically acceptable salts thereof, which are useful as inhibitors of NAMPT or ROCK, the compounds having Formula (Ic)

wherein

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R⁴ aryl and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, OR^(B), SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁷, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, NHR¹¹, N(R¹¹)₂, C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, NHSO₂R¹¹, NHC(O)OR¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, NHC(O)NH₂, NHC(O)NHR¹¹, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁸, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁸ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R¹²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹¹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹², at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹² alkyl, alkenyl, and alkynyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I; wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy;

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

Another embodiment pertains to compounds having Formula (Vc), and pharmaceutically acceptable salts thereof

wherein

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, Se, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁶, NR¹⁶C(O)R¹⁶, NHSO₂R¹⁶, NHC(O)OR¹⁶, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

Another embodiment pertains to compounds having Formula (Ic) or Formula (Vc), and pharmaceutically acceptable salts thereof; wherein X¹, X², and X³ are CH, or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹.

Another embodiment pertains to compounds having Formula (Ic) or Formula (Vc), and pharmaceutically acceptable salts thereof; wherein X¹ and X³ are CH; and X² is N; or X² is CH; and X¹ and X³ are N; X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N.

Another embodiment pertains to compounds having Formula (Ic), and pharmaceutically acceptable salts thereof, wherein R² is phenyl which is substituted at the para position with R⁵; and R⁵ is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one, or isoindolin-1-onyl.

Still another embodiment pertains to compounds of Formula (Ic), which are

-   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(furo[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(thieno[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dihydro-1,4-benzodioxin-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-fluoro-5-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-acetylphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,3-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(6-aminohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-benzodioxol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dihydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-propoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-2-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methyl-1H-indazol-5-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     5-({4[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}amino)-1H-indazole-3-carboxylate; -   N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(5-chloropyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-fluorobenzoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methoxy-1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-propoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(dimethylamino)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoro-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1,3-benzodioxol-5-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-{4-[(2-phenoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-hydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({1-[(3S)-tetrahydrofuran-3-yl]-1H-pyrazol-4-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,4-dioxa-8-azaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylthio)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(trifluoromethyl)thio]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-fluorophenyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(hydroxymethyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-benzodioxol-5-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-isopropyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiomorpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzylpiperidin-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-acetamido-2-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[3-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-imidazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-(3-cyanophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(2-hydroxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyanomethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclohexylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1H-indol-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(phenylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(diethylamino)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-phenylethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-aminophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl(1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}piperidin-4-yl)carbamate; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(cyclohexylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-chlorobenzyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(diethylcarbamoyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-hydroxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-6-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-fluoropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylmethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3,4,9-tetrahydro-2H-beta-carbolin-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tert-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[4-(trifluoromethyl)phenyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-difluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-benzylpyrrolidin-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-carbamoylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopropylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(methylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dioxolan-2-ylmethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(4-fluorophenyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-phenyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(sec-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(ethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isobutyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(trifluoromethyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,6-dimethylmorpholin-4-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(prop-2-yn-1-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyanoethyl)(cyclopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(isopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-N-isopropyl-beta-alanine; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5,6-dimethoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-chlorophenoxy)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate; -   2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic     acid; -   5-amino-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(aminomethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(2-hydroxy-2-methylpropanoyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetamido-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(N,N-dimethylglycyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methoxyacetyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methylsulfonyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4,4,4-trifluorobutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpentanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(benzyloxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[N-(2-furoyl)glycyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-thienyl)butanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-oxo-4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(N-benzoylglycyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenoxybutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propionylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(heptanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pent-4-enoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-methylpiperazin-1-yl)propanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate; -   2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic     acid; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyclopentylethyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate; -   N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1E)-5-phenylpent-1-en-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[6-(1-propyl-1H-pyrazol-4-yl)pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[1-(3-methylbutyl)-1H-pyrazol-4-yl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-phenylpentyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[2-fluoro-4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{2-fluoro-4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(isopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(isopropylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(benzoylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(butyrylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperazine-1-carboxylate; -   N-[4-(4-propionylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopropylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-butyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-isobutyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-benzoyl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[2-(3-methylbutyl)-2,3-dihydro-1H-isoindol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexyloxy)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[6-(4-chlorophenoxy)hexyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(piperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N,N′-hexane-1,6-diylbis(1,3-dihydro-2H-isoindole-2-carboxamide); -   N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   ethyl 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoate; -   N-hexyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-octyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(1-methyl-1H-pyrazol-4-yl)amino]-6-oxohexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[6-(methylamino)-6-oxohexyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-oxo-6-[(3-phenylpropyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-methylbutyl)amino]-6-oxohexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(5-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-phenylpropyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-phenylpropyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(8-fluoro-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(morpholin-4-ylmethyl)-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-4,5-dihydro-3H-2,3-benzodiazepin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(1-methylpiperidin-4-yl)oxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3R)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3S)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(azetidin-1-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperidine-1-carboxylate; -   N-[4-(5-propyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[5-(3-methylbutyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-benzyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-chloropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-oxopyrrolidin-1-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-hydroxycyclopropyl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]-1H-benzimidazol-2-yl}piperazine-1-carboxylate; -   N-[2-(piperazin-1-yl)-1H-benzimidazol-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-vinyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-benzoylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(tetrahydrofuran-3-yl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-(4-{[(3-phenylpropyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-{4-[1-(4-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(tetrahydrofuran-3-ylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2S)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2R)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-phenylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-methoxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-4-yl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-(2-methoxyethyl)-N²-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-(4-cyanophenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(trifluoromethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(tetrahydrofuran-3-ylmethyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(1,2-dihydroxyethyl)-N-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-butyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide;     and -   N-[2-(4-acetylpiperazin-1-yl)-1H-benzimidazol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-D-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propionyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-chlorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-furoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-thienylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrrol-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2,5-dimethyl-1H-pyrrol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,3-thiazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isonicotinoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridazin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrimidin-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(piperidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[6-(benzoylamino)hexyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(benzoylamino)methyl]benzyl}carbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-L-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-D-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(1-acetylpiperidin-4-yl)carbonyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-acetamidobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(methylsulfonyl)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-butyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isobutyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methylbutanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,3,3-trifluoropropanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(methoxyacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopentylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclohexylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[3-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,4-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,5-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(3,4-dimethoxyphenyl)acetyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrrol-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrazol-5-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isonicotinoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridazin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrazin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrimidin-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(N,N-dimethyl-beta-alanyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-acetylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1,3-thiazol-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(morpholin-4-ylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide;     N-[1-(2-phenylethyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-[2-(dimethylamino)ethyl]-N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(morpholin-4-ylcarbonyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{benzyl[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutoxycarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     4-{[(5-cyano-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoate; -   N-(4-{(E)-[(benzyloxy)imino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-aminopyrrolidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-methylbutyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-phenylpropyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-[4-({benzyl[3-(morpholin-4-yl)propyl]amino}methyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-methyl-1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-methoxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-hydroxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(aminomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide;

N-(4-{[(2S)-1-hydroxy-4-(methylthio)butan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;

N-(4-{[(2S,3S)-1-hydroxy-3-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;

-   N-(4-{[(2S)-1-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3R)-1,3-dihydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxyhexan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2R)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-cyclohexyl-3-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({(2R)-1-hydroxy-3-[(4-methylbenzyl)thio]propan-2-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-tert-butylphenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methoxy-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[6-(benzoylamino)hexyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(2-methoxyethoxy)acetyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]pyrazin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-acetamidohexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(1E)-3-[benzyl(methyl)amino]prop-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-phenoxypiperidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-phenoxyazetidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[benzyl(methyl)amino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[2-(2-oxopyrrolidin-1-yl)ethyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1-benzylpiperidin-4-yl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(morpholin-4-yl)benzyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxypropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-3-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{1′-[(2-methoxyethoxy)acetyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[4-(methylsulfonyl)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(ethoxyacetyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(cyclopentylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-hydroxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-hydroxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-hydroxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-methoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-methoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-methoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-fluorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-fluorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-fluorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-chlorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-chlorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-chlorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-cyanobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-cyanobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[3-(dimethylamino)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[4-(dimethylamino)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[3-(trifluoromethyl)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[4-(trifluoromethyl)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[3-(trifluoromethoxy)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2,3-dimethoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2,4-dimethoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2,5-dimethoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(phenylacetyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(3-fluorophenyl)acetyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(morpholin-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[6-(benzoylamino)hexyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   4-fluoro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-cyano-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(pyridin-2-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1-methylpyrrolidin-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(7-oxo-7-{[(3R)-tetrahydrofuran-3-ylmethyl]amino}heptyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{7-oxo-7-[(tetrahydro-2H-pyran-4-ylmethyl)amino]heptyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(azetidin-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(morpholin-4-ylmethyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methylpiperazin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(3-methylbutyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-hydroxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-chlorobenzoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1-methylpyrrolidin-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-aminoethyl)-1H-imidazol-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2,2-dimethyl-1,3-dioxolan-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-methoxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}-2-oxoethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-{benzyl[3-(morpholin-4-yl)propyl]amino}-3-oxopropyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide;     N-[4-(6-bromo-2-oxoquinolin-1(2H)-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[6-(3-acetylphenyl)-2-oxoquinolin-1(2H)-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(morpholin-4-ylacetyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(morpholin-4-ylacetyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazol-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2-benzyl-1,3-thiazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(7-{benzyl[3-(morpholin-4-yl)propyl]amino}-7-oxoheptyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-thiazol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(4-methylphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-dihydroxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(ethylsulfonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2,3-dihydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1-hydroxy-4-methylpentan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(5-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.3]hept-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.4]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,9-diazaspiro[5.5]undec-3-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{benzyl[3-(morpholin-4-yl)propyl]amino}-4-oxobutyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-phenylbutyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetyl-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-hydroxyethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butyrylamino)phenyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methoxybenzyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(2-oxa-7-azaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5     (3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydrofuro[3,4-c]pyridin-5     (3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[6-(3-acetylphenyl)-4-(3-hydroxypropyl)-2-oxoquinolin-1(2H)-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-(acetamidomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[2-(2-chlorobenzyl)-1,3-thiazol-4-yl]-2-thienyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-fluorophenyl)butyl]-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(2-hydroxypropan-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     {4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzyl}carbamate; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(methoxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(tetrahydrofuran-2-ylmethyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methoxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[4-(2-methoxyethyl)piperazin-1-yl]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-pentanoylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butyrylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(1-acetylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(1-isobutyrylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(3-methylbutanoyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(methoxyacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl(2-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}ethyl)carbamate; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-phenylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxyphenyl)acetyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-benzoylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-ethoxypropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl[(1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}azetidin-3-yl)methyl]carbamate; -   N-(4-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(morpholin-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2-methoxyethoxy)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(2,3-dimethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxycyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[4-(acetylamino)phenyl]sulfonyl}amino)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(propylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-propylphenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(butylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[({[(1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methyl}sulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(benzylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-fluorophenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(thiophen-2-ylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(N,N-dimethylglycyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(4,4-difluorocyclohexyl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-(4-{[1-(1,3-thiazol-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-D-phenylalaninamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(5-methyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-carbamoylbenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   Nalpha-{4-[(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(4,5,6,7-tetrahydro-1H-indazol-5-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   5-fluoro-N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanocyclopropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   methyl     1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate; -   N-(4-{3-[(3-methylbutyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydrofuran-2-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(benzylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(cyclopentylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(cyclopentylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(2-methoxyethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrrolidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[(dimethylamino)methyl]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-oxazol-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorobenzyl)(3-methylbutanoyl)amino]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[7-chloro-1-(2-hydroxyethyl)-3-oxo-1,3-dihydrocyclobuta[c]quinolin-4(2H)-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4[(1-acetylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butanoylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-difluoroethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiophen-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pyrimidin-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-acetylpiperidin-4-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{7-oxo-7-[(3-phenylpropyl)amino]heptyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1,3-thiazol-5-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-oxo-4,5,6,7-tetrahydro-1-benzofuran-3-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{2-[(3-methylbutanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(4-methylpentanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(ethoxyacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{[(2-methoxyethoxy)acetyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-2-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[2-(benzoylamino)ethyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-3-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-propanoylazetidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pent-4-ynoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethylglycyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethyl-beta-alanyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrrolidin-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(pyrrolidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methylpiperazin-1-yl)acetyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopropylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopentylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(butylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-fluorophenyl)sulfonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propan-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(benzylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4,4-difluoro     cyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-D-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpentanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridazin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     N-(4-{[1-(pyrimidin-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   benzyl     trans-3-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]cyclobutanecarboxylate; -   N-[4-(4-{[(4-methylpiperazin-1-yl)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(benzoylamino)cyclohex-1-en-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1-methylpiperidin-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3R)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3S)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-2-methylbutanoyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(3-methylbutanoyl)amino]oxetan-3-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   tert-butyl     4-({4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}sulfonyl)piperidine-1-carboxylate; -   N-{4-[4-(propylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methoxyethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclopentylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(1,4-dioxan-2-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopentylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(morpholin-4-ylcarbonyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopropylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(butan-2-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{(4R)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(4S)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[trans-3-(benzylcarbamoyl)cyclobutyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{trans-3-[(2-phenylethyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{trans-3-[(3-phenylpropyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methyl-1,3-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(furan-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-3-(furan-2-yl)prop-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,3-oxazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3,3,3-trifluoropropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,5-dimethyl-1H-pyrazol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methoxycyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-difluorocyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1H-pyrazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tert-butoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-1,2,4-triazol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-ethoxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-hydroxy-3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-pyrrol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methylpropoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1-methylprolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-hydroxycyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-{[1-(methoxymethyl)cyclopropyl]carbonyl}-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(methylsulfonyl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-4-methylpent-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-methoxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopent-1-en-1-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(thiophen-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-propanoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4-methylhexanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-dimethylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclobutylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(piperidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[2-(pyrrolidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(bicyclo[2.2.1]hept-2-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopentylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds of Formula (Ic), which are

-   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds of Formula (Ic), which are

-   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Another embodiment pertains to a composition for treating hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, spinal-cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, Alzheimer's disease, pain, multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, preterm labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive compulsive disorder and bipolar disorder, epilepsy and seizure disorders, for decreasing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for the prevention of graft failure, and cystic fibrosis, said composition comprising an excipient and a therapeutically effective amount of a compound of Formula (Ic), or pharmaceutically acceptable salts thereof.

Another embodiment pertains to a composition for treating inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia, said composition comprising an excipient and a therapeutically effective amount of a compound of Formula (Ic), or pharmaceutically acceptable salts thereof.

Another embodiment pertains to a method of treating hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, spinal-cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, Alzheimer's disease, pain, multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, preterm labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive compulsive disorder and bipolar disorder, epilepsy and seizure disorders, for decreasing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for the prevention of graft failure, and cystic fibrosis, in a patient, said method comprising administering to the patient a therapeutically effective amount of a compound of Formula (Ic), or pharmaceutically acceptable salts thereof.

Another embodiment pertains to a method of treating inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia in a patient, said method comprising administering to the patient a therapeutically effective amount of a compound of Formula (Ic), or pharmaceutically acceptable salts thereof.

Another embodiment pertains to a method of treating hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, spinal-cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, Alzheimer's disease, pain, multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, preterm labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive compulsive disorder and bipolar disorder, epilepsy and seizure disorders, for decreasing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for the prevention of graft failure, and cystic fibrosis in a patient, said method comprising administering to the patient therapeutically effective amount of the compound of Formula (Ic), or pharmaceutically acceptable salts thereof; and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Another embodiment pertains to a method of treating inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia or spleen cancer in a patient, said method comprising administering to the patient therapeutically effective amount of the compound of Formula (Ic), or pharmaceutically acceptable salts thereof; and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

DETAILED DESCRIPTION OF THE INVENTION

This detailed description is intended only to acquaint others skilled in the art with Applicants' invention, its principles, and its practical application so that others skilled in the art may adapt and apply the invention in its numerous forms, as they may be best suited to the requirements of a particular use. This description and its specific examples are intended for purposes of illustration only. This invention, therefore, is not limited to the embodiments described in this patent application, and may be variously modified.

Abbreviations and Definitions

Unless otherwise defined herein, scientific and technical terms used in connection with the present invention shall have the meanings that are commonly understood by those of ordinary skill in the art. The meaning and scope of the terms should be clear, however, in the event of any latent ambiguity, definitions provided herein take precedent over any dictionary or extrinsic definition. In this application, the use of “or” means “and/or” unless stated otherwise. Furthermore, the use of the term “including”, as well as other forms, such as “includes” and “included”, is not limiting. With reference to the use of the words “comprise” or “comprises” or “comprising” in this patent application (including the claims), Applicants note that unless the context requires otherwise, those words are used on the basis and clear understanding that they are to be interpreted inclusively, rather than exclusively, and that Applicants intend each of those words to be so interpreted in construing this patent application, including the claims below. For a variable that occurs more than one time in any substituent or in the compound of the invention or any other formulae herein, its definition on each occurrence is independent of its definition at every other occurrence. Combinations of substituents are permissible only if such combinations result in stable compounds. Stable compounds are compounds which can be isolated in a useful degree of purity from a reaction mixture.

It is meant to be understood that proper valences are maintained for all combinations herein, that monovalent moieties having more than one atom are attached through their left ends, and that divalent moieties are drawn from left to right.

As used in the specification and the appended claims, unless specified to the contrary, the following terms have the meaning indicated:

The term “alkyl” (alone or in combination with another term(s)) means a straight- or branched-chain saturated hydrocarbyl substituent typically containing from 1 to about 10 carbon atoms; or in another embodiment, from 1 to about 8 carbon atoms; in another embodiment, from 1 to about 6 carbon atoms; and in another embodiment, from 1 to about 4 carbon atoms. Examples of such substituents include methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, iso-amyl, and hexyl and the like.

The term “alkenyl” (alone or in combination with another term(s)) means a straight- or branched-chain hydrocarbyl substituent containing one or more double bonds and typically from 2 to about 10 carbon atoms; or in another embodiment, from 2 to about 8 carbon atoms; in another embodiment, from 2 to about 6 carbon atoms; and in another embodiment, from 2 to about 4 carbon atoms. Examples of such substituents include ethenyl (vinyl), 2-propenyl, 3-propenyl, 1,4-pentadienyl, 1,4-butadienyl, 1-butenyl, 2-butenyl, and 3-butenyl and the like.

The term “alkynyl” (alone or in combination with another term(s)) means a straight- or branched-chain hydrocarbyl substituent containing one or more triple bonds and typically from 2 to about 10 carbon atoms; or in another embodiment, from 2 to about 8 carbon atoms; in another embodiment, from 2 to about 6 carbon atoms; and in another embodiment, from 2 to about 4 carbon atoms. Examples of such substituents include ethynyl, 2-propynyl, 3-propynyl, 2-butynyl, and 3-butynyl and the like.

The term “carbocyclyl” (alone or in combination with another term(s)) means a saturated cyclic (i.e., “cycloalkyl”), partially saturated cyclic (i.e., “cycloalkenyl”), or completely unsaturated (i.e., “aryl”) hydrocarbyl substituent containing from 3 to 14 carbon ring atoms (“ring atoms” are the atoms bound together to form the ring or rings of a cyclic substituent). A carbocyclyl may be a single-ring (monocyclic) or polycyclic ring structure.

A carbocyclyl may be a single ring structure, which typically contains from 3 to 8 ring atoms, more typically from 3 to 6 ring atoms, and even more typically 5 to 6 ring atoms. Examples of such single-ring carbocyclyls include cyclopropyl (cyclopropanyl), cyclobutyl (cyclobutanyl), cyclopentyl (cyclopentanyl), cyclopentenyl, cyclopentadienyl, cyclohexyl (cyclohexanyl), cyclohexenyl, cyclohexadienyl, and phenyl. A carbocyclyl may alternatively be polycyclic (i.e., may contain more than one ring). Examples of polycyclic carbocyclyls include bridged, fused, and spirocyclic carbocyclyls. In a spirocyclic carbocyclyl, one atom is common to two different rings. An example of a spirocyclic carbocyclyl is spiropentanyl. In a bridged carbocyclyl, the rings share at least two common non-adjacent atoms. Examples of bridged carbocyclyls include bicyclo[2.2.1]heptanyl, bicyclo[2.2.1]hept-2-enyl, and adamantanyl. In a fused-ring carbocyclyl system, two or more rings may be fused together, such that two rings share one common bond. Examples of two- or three-fused ring carbocyclyls include naphthalenyl, tetrahydronaphthalenyl (tetralinyl), indenyl, indanyl (dihydroindenyl), anthracenyl, phenanthrenyl, and decalinyl.

The term “cycloalkyl” (alone or in combination with another term(s)) means a saturated cyclic hydrocarbyl substituent containing from 3 to 14 carbon ring atoms. A cycloalkyl may be a single carbon ring, which typically contains from 3 to 8 carbon ring atoms and more typically from 3 to 6 ring atoms. Examples of single-ring cycloalkyls include cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. A cycloalkyl may alternatively be polycyclic or contain more than one ring. Examples of polycyclic cycloalkyls include bridged, fused, and spirocyclic carbocyclyls. In a bridged cycloalkyl, the rings share at least two common non-adjacent atoms. Examples of bridged cycloalkyls include bicyclo[2.2.1]heptanyl and adamantanyl.

The term “aryl” (alone or in combination with another term(s)) means an aromatic carbocyclyl containing from 6 to 14 carbon ring atoms. An aryl may be monocyclic or polycyclic (i.e., may contain more than one ring). In the case of polycyclic aromatic rings, only one ring in the polycyclic system is required to be unsaturated while the remaining ring(s) may be saturated, partially saturated or unsaturated. Examples of aryls include phenyl, naphthalenyl, indenyl, 2,3-dihydroindenyl, indanyl, and tetrahydronapthyl.

In some instances, the number of carbon atoms in a hydrocarbyl substituent (e.g., alkyl, alkenyl, alkynyl, or cycloalkyl) is indicated by the prefix “C_(x)-C_(y)-”, wherein x is the minimum and y is the maximum number of carbon atoms in the substituent. Thus, for example, “C₁-C₆-alkyl” refers to an alkyl substituent containing from 1 to 6 carbon atoms. Illustrating further, C₃-C₈-cycloalkyl means a saturated hydrocarbyl ring containing from 3 to 8 carbon ring atoms.

The term “hydrogen” (alone or in combination with another term(s)) means a hydrogen radical, and may be depicted as —H.

The term “hydroxy” (alone or in combination with another term(s)) means —OH.

The term “carboxy” (alone or in combination with another term(s)) means —C(O)—OH.

The term “amino” (alone or in combination with another term(s)) means —NH₂.

The term “halogen” or “halo” (alone or in combination with another term(s)) means a fluorine radical (which may be depicted as —F), chlorine radical (which may be depicted as —Cl), bromine radical (which may be depicted as —Br), or iodine radical (which may be depicted as —I).

If a substituent is described as being “substituted”, a non-hydrogen radical is in the place of hydrogen radical on a carbon or nitrogen of the substituent. Thus, for example, a substituted alkyl substituent is an alkyl substituent in which at least one non-hydrogen radical is in the place of a hydrogen radical on the alkyl substituent. To illustrate, monofluoroalkyl is alkyl substituted with a fluoro radical, and difluoroalkyl is alkyl substituted with two fluoro radicals. It should be recognized that if there are more than one substitution on a substituent, each non-hydrogen radical may be identical or different (unless otherwise stated).

If a substituent is described as being “optionally substituted”, the substituent may be either (1) not substituted or (2) substituted. If a substituent is described as being optionally substituted with up to a particular number of non-hydrogen radicals, that substituent may be either (1) not substituted; or (2) substituted by up to that particular number of non-hydrogen radicals or by up to the maximum number of substitutable positions on the substituent, whichever is less. Thus, for example, if a substituent is described as a heteroaryl optionally substituted with up to 3 non-hydrogen radicals, then any heteroaryl with less than 3 substitutable positions would be optionally substituted by up to only as many non-hydrogen radicals as the heteroaryl has substitutable positions. To illustrate, tetrazolyl (which has only one substitutable position) would be optionally substituted with up to one non-hydrogen radical. To illustrate further, if an amino nitrogen is described as being optionally substituted with up to 2 non-hydrogen radicals, then a primary amino nitrogen will be optionally substituted with up to 2 non-hydrogen radicals, whereas a secondary amino nitrogen will be optionally substituted with up to only 1 non-hydrogen radical.

This patent application uses the terms “substituent” and “radical” interchangeably.

The prefix “halo” indicates that the substituent to which the prefix is attached is substituted with one or more independently selected halogen radicals. For example, haloalkyl means an alkyl substituent in which at least one hydrogen radical is replaced with a halogen radical. Examples of haloalkyls include chloromethyl, 1-bromoethyl, fluoromethyl, difluoromethyl, trifluoromethyl, and 1,1,1-trifluoroethyl. It should be recognized that if a substituent is substituted by more than one halogen radical, those halogen radicals may be identical or different (unless otherwise stated).

The prefix “perhalo” indicates that every hydrogen radical on the substituent to which the prefix is attached is replaced with independently selected halogen radicals, i.e., each hydrogen radical on the substituent is replaced with a halogen radical. If all the halogen radicals are identical, the prefix typically will identify the halogen radical. Thus, for example, the term “perfluoro” means that every hydrogen radical on the substituent to which the prefix is attached is substituted with a fluorine radical. To illustrate, the term “perfluoroalkyl” means an alkyl substituent wherein a fluorine radical is in the place of each hydrogen radical.

The term “carbonyl” (alone or in combination with another term(s)) means —C(O)—.

The term “aminocarbonyl” (alone or in combination with another term(s)) means —C(O)—NH₂.

The term “oxo” (alone or in combination with another term(s)) means (═O).

The term “oxy” (alone or in combination with another term(s)) means an ether substituent, and may be depicted as —O—.

The term “alkylhydroxy” (alone or in combination with another term(s)) means alkyl-OH.

The term “alkylamino” (alone or in combination with another term(s)) means alkyl-NH₂.

The term “alkyloxy” (alone or in combination with another term(s)) means an alkylether substituent, i.e., —O-alkyl. Examples of such a substituent include methoxy (—O—CH₃), ethoxy, n-propoxy, isopropoxy, n-butoxy, iso-butoxy, sec-butoxy, and tert-butoxy.

The term “alkylcarbonyl” (alone or in combination with another term(s)) means —C(O)-alkyl.

The term “aminoalkylcarbonyl” (alone or in combination with another term(s)) means —C(O)-alkyl-NH₂.

The term “alkyloxycarbonyl” (alone or in combination with another term(s)) means —C(O)—O-alkyl.

The term “carbocyclylcarbonyl” (alone or in combination with another term(s)) means —C(O)-carbocyclyl.

Similarly, the term “heterocyclylcarbonyl” (alone or in combination with another term(s)) means —C(O)-heterocyclyl.

The term “carbocyclylalkylcarbonyl” (alone or in combination with another term(s)) means —C(O)-alkyl-carbocyclyl.

Similarly, the term “heterocyclylalkylcarbonyl” (alone or in combination with another term(s)) means —C(O)-alkyl-heterocyclyl.

The term “carbocyclyloxycarbonyl” (alone or in combination with another term(s)) means —C(O)—O-carbocyclyl.

The term “carbocyclylalkyloxycarbonyl” (alone or in combination with another term(s)) means —C(O)—O-alkyl-carbocyclyl.

The term “thio” or “thia” (alone or in combination with another term(s)) means a thiaether substituent, i.e., an ether substituent wherein a divalent sulfur atom is in the place of the ether oxygen atom. Such a substituent may be depicted as —S—. This, for example, “alkyl-thio-alkyl” means alkyl-S-alkyl (alkyl-sulfanyl-alkyl).

The term “thiol” or “sulfhydryl” (alone or in combination with another term(s)) means a sulfhydryl substituent, and may be depicted as —SH.

The term “(thiocarbonyl)” (alone or in combination with another term(s)) means a carbonyl wherein the oxygen atom has been replaced with a sulfur. Such a substituent may be depicted as —C(S)—.

The term “sulfonyl” (alone or in combination with another term(s)) means —S(O)₂—.

The term “aminosulfonyl” (alone or in combination with another term(s)) means —S(O)₂—NH₂.

The term “sulfinyl” or “sulfoxido” (alone or in combination with another term(s)) means —S(O)—.

The term “heterocyclyl” (alone or in combination with another term(s)) means a saturated (i.e., “heterocycloalkyl”), partially saturated (i.e., “heterocycloalkenyl”), or completely unsaturated (i.e., “heteroaryl”) ring structure containing a total of 3 to 20 ring atoms. At least one of the ring atoms is a heteroatom (i.e., oxygen, nitrogen, or sulfur), with the remaining ring atoms being independently selected from the group consisting of carbon, oxygen, nitrogen, and sulfur. A heterocyclyl may be a single-ring (monocyclic) or polycyclic ring structure.

A heterocyclyl may be a single ring, which typically contains from 3 to 7 ring atoms, more typically from 3 to 6 ring atoms, and even more typically 5 to 6 ring atoms. Examples of single-ring heterocyclyls include 1,2,3,6-tetrahydropyridine, thiomorpholinyl, tetrahydropyranyl, furanyl, dihydrofuranyl, tetrahydrofuranyl, thiophenyl (thiofuranyl), dihydrothiophenyl, tetrahydrothiophenyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, pyrrolidin-2-onyl, imidazolyl, imidazolinyl, imidazolidinyl, pyrazolyl, pyrazolinyl, pyrazolidinyl, triazolyl, tetrazolyl, oxazolyl, oxazolidinyl, isoxazolidinyl, isoxazolyl, thiazolyl, isothiazolyl, thiazolinyl, isothiazolinyl, thiazolidinyl, isothiazolidinyl, thiodiazolyl, oxadiazolyl (including 1,2,3-oxadiazolyl, 1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl(furazanyl), or 1,3,4-oxadiazolyl), oxatriazolyl (including 1,2,3,4-oxatriazolyl or 1,2,3,5-oxatriazolyl), dioxazolyl (including 1,2,3-dioxazolyl, 1,2,4-dioxazolyl, 1,3,2-dioxazolyl, or 1,3,4-dioxazolyl), oxathiazolyl, oxathiolyl, oxathiolanyl, pyranyl, dihydropyranyl, thiopyranyl, tetrahydrothiopyranyl, pyridinyl (azinyl), piperidinyl, diazinyl (including pyridazinyl (1,2-diazinyl), pyrimidinyl (1,3-diazinyl), or pyrazinyl (1,4-diazinyl)), piperazinyl, pyrrolidin-2-only, triazinyl (including 1,3,5-triazinyl, 1,2,4-triazinyl, and 1,2,3-triazinyl)), oxazinyl (including 1,2-oxazinyl, 1,3-oxazinyl, or 1,4-oxazinyl)), oxathiazinyl (including 1,2,3-oxathiazinyl, 1,2,4-oxathiazinyl, 1,2,5-oxathiazinyl, or 1,2,6-oxathiazinyl)), oxadiazinyl (including 1,2,3-oxadiazinyl, 1,2,4-oxadiazinyl, 1,4,2-oxadiazinyl, or 1,3,5-oxadiazinyl)), morpholinyl, azepinyl, oxepinyl, thiepinyl, diazepinyl, thiomorpholinyl, tetrahydrothiophenyl 1,1-dioxidyl, tetrahydro-2H-thiopyranyl, 1,1-dioxidyl, oxetanyl, azetidinyl, thiazolyl, azepanyl, azepan-2-onyl, and dioxolayl (including 1,3-dioxolanyl).

A heterocyclyl may alternatively be polycyclic (i.e., may contain more than one ring). Examples of polycyclic heterocyclyls include bridged, fused, and spirocyclic heterocyclyls. In a spirocyclic heterocyclyl, one atom is common to two different rings. In a bridged heterocyclyl, the rings share at least two common non-adjacent atoms. In a fused-ring heterocyclyl, two or more rings may be fused together, such that two rings share one common bond. Examples of fused ring heterocyclyls containing two, three or four rings include hexahydro-furo[3,4-c]pyrrole, hexahydro-furo[3,4-b]pyrrole, octahydro-pyrrolo[3,4-b]pyridine, octahydro-pyrrolo[3,4-c]pyridine, (3aR,6aR)-5-methyl-octahydro-pyrrolo[3,4-b]pyrrole, (3aR,6aR)-octahydro-pyrrolo[3,4-b]pyrrole, 6-methyl-2,6-diazabicyclo[3.2.0]heptane, (3aS,6aR)-2-methyl-octahydro-pyrrolo[3,4-c]pyrrole, decahydro-[1,5]naphthyridine, 2,3-dihydrobenzofuranyl, 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indolyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, isoindolin-1-onyl, phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, (trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-onyl, 1,2,3,4-tetrahydroisoquinolinyl, 2,3-dihydrobenzo[b][1,4]dioxinyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl, 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, indolizinyl, pyranopyrrolyl, 4H-quinolizinyl, purinyl, naphthyridinyl, pyridopyridinyl (including pyrido[3,4-b]-pyridinyl, pyrido[3,2-b]-pyridinyl, or pyrido[4,3-b]-pyridinyl), pteridinyl, 4,5,6,7-tetrahydro-indolyl, 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazinyl, 6,7-dihydropyrrolo[3,4-d]pyrimidinyl, 6,7-dihydropyrrolo[3,4-b]pyridinyl, 2,3-dihydropyrrolo[3,4-c]pyridinyl, 6,7-dihydrobenzofuran-4(5H)-onyl, indolinyl, benzo[d][1,3]dioxolyl, isoquinolinyl, indolyl, quinolin-2(1H)-onyl, benzo[d]imidazolyl, 1,2,3,4-tetrahydrocyclobuta[c]quinolinyl, 1,2-dihydrocyclobuta[c]quinolin-3(4H)-onyl, and 3,3a,4,4a-tetrahydro-2H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-5(6H)-onyl. Other examples of fused-ring heterocyclyls include benzo-fused heterocyclyls, such as benzimidazolyl, benzo[d][1,3]dioxolyl, indolyl, isoindolyl (isobenzazolyl, pseudoisoindolyl), indoleninyl (pseudoindolyl), isoindazolyl (benzpyrazolyl), benzazinyl (including quinolinyl (1-benzazinyl) or isoquinolinyl (2-benzazinyl)), phthalazinyl, quinoxalinyl, quinazolinyl, benzodiazinyl (including cinnolinyl (1,2-benzodiazinyl) or quinazolinyl (1,3-benzodiazinyl)), benzopyranyl (including chromanyl or isochromanyl), benzoxazinyl (including 1,3,2-benzoxazinyl, 1,4,2-benzoxazinyl, 2,3,1-benzoxazinyl, or 3,1,4-benzoxazinyl), benzisoxazinyl (including 1,2-benzisoxazinyl or 1,4-benzisoxazinyl), isoindolin-1-onyl, 2,3-dihydrobenzo[b][1,4]dioxinyl, 1,2,3,4-tetrahydroisoquinolinyl, quinolin-2(1H)-onyl, benzo[d]imidazolyl, 2,3,4,9-tetrahydro-pyrido[3,4-b]indolyl, 1,2,3,4-tetrahydrocyclobuta[c]quinolinyl, 1,2-dihydrocyclobuta[c]quinolin-3(4H)-onyl, and 3,3a,4,4a-tetrahydro-2H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-5(6H)-onyl. Examples of spirocyclic heterocyclyls include 1,4-dioxa-8-azaspiro[4.5]decanyl, 2-oxa-6-aza-spiro[3.3]heptanyl, bicyclo[2.2.1]heptan-2-only, 6-oxa-1-aza-spiro[3.3]heptanyl, 2-oxa-7-aza-spiro[3.5]nonanyl, 2-oxa-6-aza-spiro[3.5]nonanyl, 2-oxa-5-aza-spiro[3.5]nonanyl, 2-oxa-6-aza-spiro[3.4]octanyl, 2-oxa-5-aza-spiro[3.4]octanyl, 2,7-diazaspiro[3.5]nonane, 1,4-dioxa-8-azaspiro[4.5]decanyl, 2-oxa-9-azaspiro[5.5]undecanyl, 2,9-diazaspiro[5.5]undecanyl, 2,8-diazaspiro[5.5]undecanyl, 1-oxa-8-azaspiro[5.5]undecanyl, 1,8-diazaspiro[5.5]undecanyl, 3,9-diazaspiro[5.5]undecanyl, 1-oxa-4,8-diazaspiro[5.5]undecanyl, 1,8-diazaspiro[4.6]undecanyl, 1-oxa-8-azaspiro[4.5]decanyl, 2,7-diazaspiro[4.5]decanyl, 1,8-diazaspiro[4.5]decanyl, 2,8-diazaspiro[4.5]decanyl, 2,6-diazaspiro[4.5]decanyl, 1,4-dioxaspiro[4.5]decanyl, 1,7-diazaspiro[4.4]nonanyl, 2,7-diazaspiro[4.4]nonanyl, 2,5-diazaspiro[3.5]nonanyl, 2,6-diazaspiro[3.5]nonanyl, 1,7-diazaspiro[3.5]nonanyl, 6-oxa-2-azaspiro[3.5]nonanyl, 1,6-diazaspiro[3.5]nonanyl, 2,6-diazaspiro[3.4]octanyl, 6-oxa-2-azaspiro[3.4]octanyl, 5-oxa-2-azaspiro[3.4]octanyl, and 2,6-diazaspiro[3.3]heptanyl.

The term “heterocycloalkyl” (alone or in combination with another term(s)) means a saturated heterocyclyl. Examples of heterocycloalkyls include piperidine, tetrahydropyranyl, piperazinyl, morpholinyl, azepan-2-oneyl, pyrrolidinyl, 1,3-dioxolanyl, tetrahydrofuranyl, pyrrolidin-2-onyl, oxetanyl, azetidinyl, 2-oxa-9-azaspiro[5.5]undecanyl, 2,9-diazaspiro[5.5]undecanyl, 2,8-diazaspiro[5.5]undecanyl, 1-oxa-8-azaspiro[5.5]undecanyl, 1,8-diazaspiro[5.5]undecanyl, 3,9-diazaspiro[5.5]undecanyl, 1-oxa-4,8-diazaspiro[5.5]undecanyl, 1,8-diazaspiro[4.6]undecanyl, 1-oxa-8-azaspiro[4.5]decanyl, 2,7-diazaspiro[4.5]decanyl, 1,8-diazaspiro[4.5]decanyl, 2,8-diazaspiro[4.5]decanyl, 2,6-diazaspiro[4.5]decanyl, 1,4-dioxaspiro[4.5]decanyl, 1,7-diazaspiro[4.4]nonanyl, 2,7-diazaspiro[4.4]nonanyl, 2,5-diazaspiro[3.5]nonanyl, 2,6-diazaspiro[3.5]nonanyl, 1,7-diazaspiro[3.5]nonanyl, 6-oxa-2-azaspiro[3.5]nonanyl, 1,6-diazaspiro[3.5]nonanyl, 2,6-diazaspiro[3.4]octanyl, 6-oxa-2-azaspiro[3.4]octanyl, 5-oxa-2-azaspiro[3.4]octanyl, bicyclo[2.2.1]heptan-2-onyl, 1,4-dioxa-8-azaspiro[4.5]decanyl, 2,7-diazaspiro[3.5]nonanyl and 2,6-diazaspiro[3.3]heptanyl.

The term “heteroaryl” (alone or in combination with another term(s)) means an aromatic heterocyclyl containing from 5 to 14 ring atoms. A heteroaryl may be monocyclic or polycyclic (i.e., may contain more than one ring). In the case of a polycyclic heteroaryl, only one heterocyclyl ring in the polycyclic system is required to be unsaturated while the remaining ring(s) may be saturated, partially saturated or unsaturated. Examples of heteroaryl substituents include: 6-membered ring substituents such as pyridyl, pyrazyl, pyrrolyl, isoxazolyl, 1,2,3-triazolyl, pyrimidinyl, pyridazinyl, and 1,3,5-, 1,2,4- or 1,2,3-triazinyl; 5-membered ring substituents such as imidazyl, furanyl, thiophenyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, 1,2,3-, 1,2,4-, 1,2,5-, and 1,3,4-, oxadiazolyl and isothiazolyl; 6/5-membered fused ring substituents such as indolyl, benzothiofuranyl, benzisoxazolyl, benzoxazolyl, purinyl, 4,5,6,7-tetrahydro-indolyl, furo[3,2-c]pyridinyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-onyl, thieno[3,2-c]pyridinyl, 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazinyl, benzo[d]imidazolyl, 6,7-dihydro-pyrrolo[3,4-d]pyrimidinyl, 6,7-dihydro-pyrrolo[3,4-b]pyridinyl, 2,3-dihydro-pyrrolo[3,4-c]pyridinyl, 5,6,7,8-tetrahydroimidazo[1,5-a]pyrazinyl, 6,7-dihydrobenzofuran-4(5H)-onyl, 6,7-dihydrobenzofuran-4(5H)-onyl, and indolyl; 6/6-membered fused rings such as benzopyranyl, quinolinyl, isoquinolinyl, cinnolinyl, quinazolinyl, benzoxazinyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, phthalazin-1(2H)-onyl, isoquinolin-1(2H)-onyl, and quinolin-2(1H)-onyl; 6/5/6 membered rings such as 2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indolyl, and 1,2-dihydrocyclobuta[c]quinolin-3(4H)-onyl; and 6/6/4/5 membered rings such as 2,3,4,9-tetrahydro-pyrido[3,4-b]indolyl.

A prefix attached to a multi-component substituent only applies to the first component. To illustrate, the term “alkylcycloalkyl” contains two components: alkyl and cycloalkyl. Thus, the C₁-C₆— prefix on C₁-C₆-alkylcycloalkyl means that the alkyl component of the alkylcycloalkyl contains from 1 to 6 carbon atoms; the C₁-C₆-prefix does not describe the cycloalkyl component. To illustrate further, the prefix “halo” on haloalkyloxyalkyl indicates that only the alkyloxy component of the alkyloxyalkyl substituent is substituted with one or more halogen radicals. If halogen substitution may alternatively or additionally occur on the alkyl component, the substituent would instead be described as “halogen-substituted alkyloxyalkyl” rather than “haloalkyloxyalkyl.” And finally, if the halogen substitution may only occur on the alkyl component, the substituent would instead be described as “alkyloxyhaloalkyl.”

The terms “treat”, “treating” and “treatment” refer to a method of alleviating or abrogating a disease and/or its attendant symptoms.

The terms “prevent”, “preventing” and “prevention” refer to a method of preventing the onset of a disease and/or its attendant symptoms or barring a subject from acquiring a disease. As used herein, “prevent”, “preventing” and “prevention” also include delaying the onset of a disease and/or its attendant symptoms and reducing a subject's risk of acquiring a disease.

The term “therapeutically effective amount” refers to that amount of the compound being administered sufficient to prevent development of or alleviate to some extent one or more of the symptoms of the condition or disorder being treated.

The term “modulate” refers to the ability of a compound to increase or decrease the function, or activity, of a kinase. “Modulation”, as used herein in its various forms, is intended to encompass antagonism, agonism, partial antagonism and/or partial agonism of the activity associated with kinase. Kinase inhibitors are compounds that, e.g., bind to, partially or totally block stimulation, decrease, prevent, delay activation, inactivate, desensitize, or down regulate signal transduction. Kinase activators are compounds that, e.g., bind to, stimulate, increase, open, activate, facilitate, enhance activation, sensitize or up regulate signal transduction.

The term “composition” as used herein is intended to encompass a product comprising the specified ingredients in the specified amounts, as well as any product which results, directly or indirectly, from combination of the specified ingredients in the specified amounts. By “pharmaceutically acceptable” it is meant the carrier, diluent or excipient must be compatible with the other ingredients of the formulation and not deleterious to the recipient thereof.

The “subject” is defined herein to include animals such as mammals, including, but not limited to, primates (e.g., humans), cows, sheep, goats, horses, dogs, cats, rabbits, rats, mice and the like. In preferred embodiments, the subject is a human.

Isotope Enriched or Labeled Compounds

Compounds of the invention can exist in isotope-labeled or -enriched form containing one or more atoms having an atomic mass or mass number different from the atomic mass or mass number most abundantly found in nature. Isotopes can be radioactive or non-radioactive isotopes. Isotopes of atoms such as hydrogen, carbon, phosphorous, sulfur, fluorine, chlorine, and iodine include, but are not limited to, ²H, ³H, ¹³C, ¹⁴C, ¹⁵N, ¹⁸O, ³²P, ³⁵S, ³⁶Cl, and ¹²⁵I. Compounds that contain other isotopes of these and/or other atoms are within the scope of this invention.

In another embodiment, the isotope-labeled compounds contain deuterium (²H), tritium (³H) or ¹⁴C isotopes. Isotope-labeled compounds of this invention can be prepared by the general methods well known to persons having ordinary skill in the art. Such isotope-labeled compounds can be conveniently prepared by carrying out the procedures disclosed in the Examples disclosed herein and Schemes by substituting a readily available isotope-labeled reagent for a non-labeled reagent. In some instances, compounds may be treated with isotope-labeled reagents to exchange a normal atom with its isotope, for example, hydrogen for deuterium can be exchanged by the action of a deuteric acid such as D₂SO₄/D₂O. In addition to the above, relevant procedures and intermediates are disclosed, for instance, in Lizondo, J et al., Drugs Fut, 21(11), 1116 (1996); Brickner, S J et al., J Med Chem, 39(3), 673 (1996); Mallesham, B et al., Org Lett, 5(7), 963 (2003); PCT publications WO1997010223, WO2005099353, WO1995007271, WO2006008754; U.S. Pat. Nos. 7,538,189; 7,534,814; 7,531,685; 7,528,131; 7,521,421; 7,514,068; 7,511,013; and US Patent Application Publication Nos. 20090137457; 20090131485; 20090131363; 20090118238; 20090111840; 20090105338; 20090105307; 20090105147; 20090093422; 20090088416; and 20090082471, the methods are hereby incorporated by reference.

The isotope-labeled compounds of the invention may be used as standards to determine the effectiveness of Bcl-2 inhibitors in binding assays. Isotope containing compounds have been used in pharmaceutical research to investigate the in vivo metabolic fate of the compounds by evaluation of the mechanism of action and metabolic pathway of the nonisotope-labeled parent compound (Blake et al. J. Pharm. Sci. 64, 3, 367-391 (1975)). Such metabolic studies are important in the design of safe, effective therapeutic drugs, either because the in vivo active compound administered to the patient or because the metabolites produced from the parent compound prove to be toxic or carcinogenic (Foster et al., Advances in Drug Research Vol. 14, pp. 2-36, Academic press, London, 1985; Kato et al., J. Labelled Comp. Radiopharmaceut., 36(10):927-932 (1995); Kushner et al., Can. J. Physiol. Pharmacol., 77, 79-88 (1999).

In addition, non-radio active isotope containing drugs, such as deuterated drugs called “heavy drugs,” can be used for the treatment of diseases and conditions related to Bcl-2 activity. Increasing the amount of an isotope present in a compound above its natural abundance is called enrichment. Examples of the amount of enrichment include from about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 21, 25, 29, 33, 37, 42, 46, 50, 54, 58, 63, 67, 71, 75, 79, 84, 88, 92, 96, to about 100 mol %. Replacement of up to about 15% of normal atom with a heavy isotope has been effected and maintained for a period of days to weeks in mammals, including rodents and dogs, with minimal observed adverse effects (Czajka D M and Finkel A J, Ann. N.Y. Acad. Sci. 1960 84: 770; Thomson J F, Ann. New York Acad. Sci 1960 84: 736; Czakja D M et al., Am. J. Physiol. 1961 201: 357). Acute replacement of as high as 15%-23% in human fluids with deuterium was found not to cause toxicity (Blagojevic N et al. in “Dosimetry & Treatment Planning for Neutron Capture Therapy”, Zamenhof R, Solares G and Harling O Eds. 1994. Advanced Medical Publishing, Madison Wis. pp. 125-134; Diabetes Metab. 23: 251 (1997)).

Stable isotope labeling of a drug can alter its physico-chemical properties such as pKa and lipid solubility. These effects and alterations can affect the pharmacodynamic response of the drug molecule if the isotopic substitution affects a region involved in a ligand-receptor interaction. While some of the physical properties of a stable isotope-labeled molecule are different from those of the unlabeled one, the chemical and biological properties are the same, with one important exception: because of the increased mass of the heavy isotope, any bond involving the heavy isotope and another atom will be stronger than the same bond between the light isotope and that atom. Accordingly, the incorporation of an isotope at a site of metabolism or enzymatic transformation will slow said reactions potentially altering the pharmacokinetic profile or efficacy relative to the non-isotopic compound.

Compounds

Suitable groups for X¹, X², X³, and R² in compounds of Formula (I) are independently selected. The described embodiments of the present invention may be combined. Such combination is contemplated and within the scope of the present invention. For example, it is contemplated that embodiments for any of X¹, X², X³, and R² can be combined with embodiments defined for any other of X¹, X², X³, and R².

Embodiments of Formula (I)

One embodiment of this invention, therefore, pertains to compounds or pharmaceutically acceptable salts, which are useful as inhibitors of NAMPT, the compounds having Formula (I)

wherein

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NH₂, NHR⁴, N(R⁴)₂, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each phenyl is optionally substituted at the para position with one independently selected R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each phenyl is optionally substituted with one F; wherein each heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein R² is not 4-methylphenyl;

R³ is alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁴ is alkyl, alkenyl, alkynyl, aryl or heterocyclyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each aryl and heterocycyl is optionally substituted with one or more independently selected R⁸, OR^(B), SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁷ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, NHR¹¹, N(R¹¹)₂, C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, SO₂N(R¹¹)₂, NHC(O)NH₂, NHC(O)NHR¹¹, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁸ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R¹²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, or aryl;

R¹⁰ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹¹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹² is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁹, R¹¹, and R¹² are optionally substituted with one or more independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, CO(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; and

R¹⁵ is alkyl.

In one embodiment of Formula (I), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N. In another embodiment of Formula (I), X¹, X², and X³ are CH. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (I), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is N.

In another embodiment of Formula (I), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (I), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), R¹ is C(O)NH₂. In another embodiment of Formula (I), R¹ is F. In another embodiment of Formula (I), R¹ is Cl. In another embodiment of Formula (I), R¹ is Br. In another embodiment of Formula (I), R¹ is CN. In another embodiment of Formula (I), R¹ is NH₂. In another embodiment of Formula (I), R¹ is NO₂. In another embodiment of Formula (I), R¹ is CF₃. In another embodiment of Formula (I), R¹ is C(O)OH.

In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (I), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (I), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (I), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH.

In one embodiment of Formula (I),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is alkyl, phenyl, heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁴, OR⁴, C(O)R⁴, CO(O)R⁴, NHC(O)R⁴, C(O)NHR⁴, F, Cl, Br or I; each phenyl is optionally substituted at the para position with one independently selected R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, C(O)R⁵, NHR⁵, NHC(O)R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, or CF₃; wherein each phenyl is optionally substituted with one F; wherein each heterocyclyl is optionally substituted with one or more independently selected R⁵, C(O)R⁵, NHC(O)R⁵, C(O)NHR⁵, F, Cl, Br or I; wherein R² is not 4-methylphenyl;

R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, OH, F, Cl, Br or I;

R⁴ is alkyl, aryl or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁷, F, Cl, Br or I; wherein each aryl and heterocycyl is optionally substituted with one or more independently selected R⁸, C(O)R⁸, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, C(O)NH₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶ is alkyl or heterocyclyl;

R⁷ is aryl;

R⁸ is alkyl, aryl, or heterocyclyl;

R⁹ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OCH₃, or aryl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, and R⁹ are optionally substituted with one or more independently selected R¹³, OR¹³SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, NH₂, OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, C(O)R¹⁵, CN, CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, aryl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OH, F, Cl, Br or I; and

R¹⁵ is alkyl.

Still another embodiment pertains to compounds having Formula (I), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 357, 358, 359, 360, 361, 362, 363, 364, 365, 366, 367, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (II)

In another aspect, the present invention provides compounds of Formula (II)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (I); and R² is phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the phenyl, heterocyclyl, cycloalkyl, and cycloalkenyl are optionally substituted as described herein for Formula (I).

In one embodiment of Formula (II), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N. In another embodiment of Formula (II), X¹, X², and X³ are CH. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (II), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is N.

In another embodiment of Formula (II), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (II), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), R¹ is C(O)NH₂. In another embodiment of Formula (II), R¹ is F. In another embodiment of Formula (II), R¹ is Cl. In another embodiment of Formula (II), R¹ is Br. In another embodiment of Formula (II), R¹ is CN. In another embodiment of Formula (II), R¹ is NH₂. In another embodiment of Formula (II), R¹ is NO₂. In another embodiment of Formula (II), R¹ is CF₃. In another embodiment of Formula (II), R¹ is C(O)OH.

In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (II), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (II), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (II), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH.

In one embodiment of Formula (II),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is phenyl, or heterocyclyl; wherein each phenyl is optionally substituted at the para position with one independently selected R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, C(O)R⁵, NHR⁵, NHC(O)R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, or CF₃; wherein each phenyl is optionally substituted with one F; wherein each heterocyclyl is optionally substituted with one or more independently selected R⁵, C(O)R⁵, NHC(O)R⁵, C(O)NHR⁵, F, Cl, Br or I; wherein R² is not 4-methylphenyl;

R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, OH, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, C(O)NH₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶ is alkyl or heterocyclyl;

R⁹ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OCH₃, or aryl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, and R⁹ are optionally substituted with one or more independently selected R¹³, OR¹³SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, NH₂, OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, C(O)R¹⁵, CN, CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, aryl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OH, F, Cl, Br or I; and

R¹⁵ is alkyl.

Still another embodiment pertains to compounds having Formula (II), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 452, 453, 454, 455, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (III)

In another aspect, the present invention provides compounds of Formula (III)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (I); and R^(X) is as described herein for Formula (I) when R² is phenyl.

In one embodiment of Formula (III), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N. In another embodiment of Formula (III), X¹, X², and X³ are CH. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (III), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is N.

In another embodiment of Formula (III), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (III), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), R¹ is C(O)NH₂. In another embodiment of Formula (III), R¹ is F. In another embodiment of Formula (III), R¹ is Cl. In another embodiment of Formula (III), R¹ is Br. In another embodiment of Formula (III), R¹ is CN. In another embodiment of Formula (III), R¹ is NH₂. In another embodiment of Formula (III), R¹ is NO₂. In another embodiment of Formula (III), R¹ is CF₃. In another embodiment of Formula (III), R¹ is C(O)OH.

In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (III), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (III), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (III), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (III), R^(x) is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, or pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one.

In one embodiment of Formula (III),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R^(X) is R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, C(O)R⁵, NHR⁵, NHC(O)R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CF₃ or F;

R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, OH, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, C(O)NH₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶ is alkyl or heterocyclyl;

R⁹ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OCH₃, or aryl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, and R⁹ are optionally substituted with one or more independently selected R¹³, OR¹³SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, NH₂, OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, C(O)R¹⁵, CN, CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, aryl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OH, F, Cl, Br or I; and

R¹⁵ is alkyl.

Still another embodiment pertains to compounds having Formula (III), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 330, 331, 332, 333, 336, 337, 338, 339, 340, 341, 342, 343, 348, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 547, 548, 549, 550, 551, 552, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IV)

In another aspect, the present invention provides compounds of Formula (IV)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (I).

In one embodiment of Formula (IV), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IV), X¹, X², and X³ are CH. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IV), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is N.

In another embodiment of Formula (IV), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IV), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), R¹ is C(O)NH₂. In another embodiment of Formula (IV), R¹ is F. In another embodiment of Formula (IV), R¹ is Cl. In another embodiment of Formula (IV), R¹ is Br. In another embodiment of Formula (IV), R¹ is CN. In another embodiment of Formula (IV), R¹ is NH₂. In another embodiment of Formula (IV), R¹ is NO₂. In another embodiment of Formula (IV), R¹ is CF₃. In another embodiment of Formula (IV), R¹ is C(O)OH.

In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IV), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IV), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IV), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH.

In one embodiment of Formula (IV),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, OH, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, C(O)NH₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶ is alkyl or heterocyclyl;

R⁹ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OCH₃, or aryl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, and R⁹ are optionally substituted with one or more independently selected R¹³, OR¹³SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, NH₂, OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, C(O)R¹⁵, CN, CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, aryl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OH, F, Cl, Br or I; and

R¹⁵ is alkyl.

Still another embodiment pertains to compounds having Formula (IV), which include Examples 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (V)

In another aspect, the present invention provides compounds of Formula (V)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (I).

In one embodiment of Formula (V), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N. In another embodiment of Formula (V), X¹, X², and X³ are CH. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (V), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is N.

In another embodiment of Formula (V), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (V), R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), R¹ is C(O)NH₂. In another embodiment of Formula (V), R¹ is F. In another embodiment of Formula (V), R¹ is Cl. In another embodiment of Formula (V), R¹ is Br. In another embodiment of Formula (V), R¹ is CN. In another embodiment of Formula (V), R¹ is NH₂. In another embodiment of Formula (V), R¹ is NO₂. In another embodiment of Formula (V), R¹ is CF₃. In another embodiment of Formula (V), R¹ is C(O)OH.

In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (V), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (V), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH.

In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (V), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH.

In one embodiment of Formula (V),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, OH, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, C(O)NH₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶ is alkyl or heterocyclyl;

R⁹ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OCH₃, or aryl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, and R⁹ are optionally substituted with one or more independently selected R¹³, OR¹³SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, or pyrrolidin-2-onyl, wherein each alkyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, NH₂, OH, F, Cl, Br or I; wherein each aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, C(O)R¹⁵, CN, CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, aryl, or cycloalkyl; wherein each alkyl is optionally substituted with one or more independently selected OH, F, Cl, Br or I; and

R¹⁵ is alkyl.

Still another embodiment pertains to compounds having Formula (V), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 176, 177, 178, 179, 180, 181, 182, 184, 185, 186, 187, 188, 189, 190, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 209, 210, 211, 213, 214, 215, 216, 217, 218, 219, 220, 221, 223, 224, 225, 226, 227, 228, 230, 231, 232, 234, 235, 236, 237, 239, 240, 243, 245, 246, 248, 249, 250, 251, 252, 253, 254, 256, 257, 258, 259, 260, 265, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 373, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 430, 431, 434, 435, 436, 437, 438, 439, 440, 441, 442, 445, 449, 450, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (Ia)

One embodiment of this invention, therefore, pertains to compounds or pharmaceutically acceptable salts, which are useful as inhibitors of NAMPT, the compounds having Formula (Ia)

wherein

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein R² is not 4-methylphenyl;

R³ is alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁴ is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R⁴ aryl and heterocycyl is optionally substituted with one or more independently selected R⁸, OR^(B), SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁷ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, NHR¹¹, N(R¹¹)₂, C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, NHSO₂R¹¹, NHC(O)OR¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, NHC(O)NH₂, NHC(O)NHR¹¹, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁸ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁸ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R¹²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

R¹⁰ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹¹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹² is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, and R¹² are optionally substituted with one or more independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl.

In one embodiment of Formula (Ia), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (Ia), X¹, X², and X³ are CH. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (Ia), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (Ia), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (Ia), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (Ia), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (Ia), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (Ia), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ia), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), R¹ is C(O)NH₂. In another embodiment of Formula (Ia), R¹ is F. In another embodiment of Formula (Ia), R¹ is Cl. In another embodiment of Formula (Ia), R¹ is Br. In another embodiment of Formula (Ia), R¹ is CN. In another embodiment of Formula (Ia), R¹ is NH₂. In another embodiment of Formula (Ia), R¹ is NO₂. In another embodiment of Formula (Ia), R¹ is CF₃. In another embodiment of Formula (Ia), R¹ is C(O)OH. In another embodiment of Formula (Ia), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ia), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ia), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ia), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In one embodiment of Formula (Ia),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is alkyl, phenyl, heterocyclyl, wherein each R² alkyl is optionally substituted with one or more independently selected R⁴, OR⁴, C(O)R⁴, CO(O)R⁴, NHC(O)R⁴, C(O)NHR⁴, or F, Cl, Br or I; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl is optionally substituted with one or more independently selected R⁵, C(O)R⁵, NHC(O)R⁵, C(O)NHR⁵, F, Cl, Br or I; wherein R² is not 4-methylphenyl;

R³ is alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, OH, F, Cl, Br or I;

R⁴ is alkyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl is optionally substituted with one or more independently selected R⁷, F, Cl, Br or I; wherein each R⁴ aryl and heterocycyl is optionally substituted with one or more independently selected R⁸, C(O)R⁸, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, C(O)NH₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶ is alkyl, or heterocyclyl;

R⁷ is aryl;

R⁸ is alkyl, aryl, or heterocyclyl;

R⁹ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁹ alkyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, and R⁹, are optionally substituted with one or more independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, or cycloalkyl; wherein each R¹³ alkyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, NH₂, N(R¹⁴)₂, NHC(O)R¹⁴, OH, CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, and cycloalkyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, CN, CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one or more independently selected OCH₃, OH, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl.

In another embodiment of Formula (Ia),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N;

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is alkyl, phenyl, heterocyclyl, wherein each R² alkyl is optionally substituted with one or more independently selected R⁴, OR⁴, C(O)R⁴, CO(O)R⁴, NHC(O)R⁴, C(O)NHR⁴, or F, Cl, Br or I; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, or CF₃; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl is optionally substituted with one or more independently selected R⁵, C(O)R⁵, NHC(O)R⁵, or C(O)NHR⁵; wherein R² is not 4-methylphenyl;

R³ is alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH;

R⁴ is alkyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl is optionally substituted with one or more R⁷; wherein each R⁴ aryl and heterocycyl is optionally substituted with one or more independently selected R⁸, C(O)R⁸, or Cl;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, C(O)NH₂, C(O)OH, OH, CN, or CF₃;

R⁶ is alkyl, or heterocyclyl;

R⁷ is aryl;

R⁸ is alkyl, aryl, or heterocyclyl;

R⁹ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁹ alkyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, and R⁹, are optionally substituted with one or more independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, or Cl;

R¹³ is alkyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, or cycloalkyl; wherein each R¹³ alkyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, NH₂, N(R¹⁴)₂, NHC(O)R¹⁴, OH, or CF₃; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, and cycloalkyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, CN, CF₃, F, or Cl;

R¹⁴ is alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one or more independently selected OCH₃, or OH; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl.

Still another embodiment pertains to compounds having Formula (Ia), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 358, 359, 360, 361, 362, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 542, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607, 608, 613, 614, 615, 616, 617, 618, 619, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663, 664, 665, 666, 667, 668, 669, 670, 671, 672, 673, 674, 675, 676, 677, 678, 679, 680, 681, 682, 683, 684, 685, 686, 687, 688, 689, 690, 691, 692, 693, 694, 695, 696, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIa)

In another aspect, the present invention provides compounds of Formula (IIa)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (Ia); and R² is phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the R² phenyl, heterocyclyl, cycloalkyl, and cycloalkenyl are optionally substituted as described herein for substituents on R² in Formula (Ia).

In one embodiment of formula (IIa),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein R² is not 4-methylphenyl;

R³ is alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

R¹⁰ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰, are optionally substituted with one or more independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl.

In one embodiment of Formula (IIa), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (Ha), X¹, X², and X³ are CH. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IIa), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IIa), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IIa), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IIa), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IIa), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IIa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (BO, R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (BO, R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ha), R¹ is C(O)NH₂. In another embodiment of Formula (IIa), R¹ is F. In another embodiment of Formula (IIa), R¹ is Cl. In another embodiment of Formula (BO, R¹ is Br. In another embodiment of Formula (IIa), R¹ is CN. In another embodiment of Formula (IIa), R¹ is NH₂. In another embodiment of Formula (IIa), R¹ is NO₂. In another embodiment of Formula (IIa), R¹ is CF₃. In another embodiment of Formula (BO, R¹ is C(O)OH. In another embodiment of Formula (IIa), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ha), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (IIa), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 614, 615, 617, 618, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 682, 683, 684, 685, 686, 687, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIIa)

In another aspect, the present invention provides compounds of Formula (IIIa)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (Ia); and R^(X) is as described herein for substituents at the para position in Formula (Ia) when R² is phenyl.

In one embodiment of formula (IIIa),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R^(x) is R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein R^(x) is not 4-methyl;

R³ is alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

R¹⁰ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰, are optionally substituted with one or more independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl.

In one embodiment of Formula (IIIa), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IIIa), X¹, X², and X³ are CH. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IIIa), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IIIa), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IIIa), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IIIa), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IIIa), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IIIa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), R¹ is C(O)NH₂. In another embodiment of Formula (IIIa), R¹ is F. In another embodiment of Formula (IIIa), R¹ is Cl. In another embodiment of Formula (IIIa), R¹ is Br. In another embodiment of Formula (IIIa), R¹ is CN. In another embodiment of Formula (IIIa), R¹ is NH₂. In another embodiment of Formula (IIIa), R¹ is NO₂. In another embodiment of Formula (IIIa), R¹ is CF₃. In another embodiment of Formula (IIIa), R¹ is C(O)OH. In another embodiment of Formula (IIIa), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In one embodiment of formula (IIIa), R^(x) is R⁵, OCH₂CH₂CH₂CH₂CH₂CH₃, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, or CF₃; wherein R^(x) is not 4-methyl. In another embodiment of formula (IIIa), R^(x) is R⁵, NHC(O)R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, or C(O)NHOR⁵; wherein R^(x) is not 4-methyl. In another embodiment of formula (IIIa), R^(x) is R⁵, and R⁵ is heterocyclyl, which is optionally substituted as described in embodiments herein.

In another embodiment of Formula (III), R^(x) is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one, isoindolin-1-onyl, or 1,2,3,6-tetrahydropyridinyl. In another embodiment of Formula (III), R^(x) is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, isoindolin-1-onyl, or pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one; which are optionally substituted as defined herein. In another embodiment of Formula (III), R^(x) is, 2,3,6-tetrahydropyridinyl; which is optionally substituted as defined herein.

Still another embodiment pertains to compounds having Formula (IIIa), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 327, 330, 331, 332, 333, 336, 337, 338, 339, 340, 341, 342, 343, 348, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 553, 554, 555, 556, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 649, 650, 682, 683, 684, 685, 686, 687, 705, 706, 707, 708, 709, 710, 716, 717, and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds having Formula (IIIa), which include Examples 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 547, 548, 549, 550, 551, 552, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IVa)

In another aspect, the present invention provides compounds of Formula (IVa)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (Ia).

In one embodiment of formula (IVa),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³ is alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

R¹⁰ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰, are optionally substituted with one or more independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl.

In one embodiment of Formula (IVa), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IVa), X¹, X², and X³ are CH. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IVa), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IVa), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IVa), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IVa), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IVa), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IVa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), R¹ is C(O)NH₂. In another embodiment of Formula (IVa), R¹ is F. In another embodiment of Formula (IVa), R¹ is Cl. In another embodiment of Formula (IVa), R¹ is Br. In another embodiment of Formula (IVa), R¹ is CN. In another embodiment of Formula (IVa), R¹ is NH₂. In another embodiment of Formula (IVa), R¹ is NO₂. In another embodiment of Formula (IVa), R¹ is CF₃. In another embodiment of Formula (IVa), R¹ is C(O)OH. In another embodiment of Formula (IVa), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVa), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVa), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVa), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (IVa), which include Examples 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 563, 564, 577, 579, 580, 581, 582, 583, 584, 596, 607, 649, 650, 682, 683, 684, 685, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (Va)

In another aspect, the present invention provides compounds of Formula (Va)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (Ia).

In one embodiment of formula (Va),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³ is alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁰, OR¹⁰, Se, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁶)₂, NHC(O)R¹⁶, NR¹⁶C(O)R¹⁶, NHSO₂R¹⁰, NHC(O)OR¹⁶, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

R¹⁰ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰, are optionally substituted with one or more independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl.

In one embodiment of Formula (Va), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (Va), X¹, X², and X³ are CH. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (Va), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (Va), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (Va), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (Va), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (Va), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (Va), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Va), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), R¹ is C(O)NH₂. In another embodiment of Formula (Va), R¹ is F. In another embodiment of Formula (Va), R¹ is Cl. In another embodiment of Formula (Va), R¹ is Br. In another embodiment of Formula (Va), R¹ is CN. In another embodiment of Formula (Va), R¹ is NH₂. In another embodiment of Formula (Va), R¹ is NO₂. In another embodiment of Formula (Va), R¹ is CF₃. In another embodiment of Formula (Va), R¹ is C(O)OH. In another embodiment of Formula (Va), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Va), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Va), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Va), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (Va), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 373, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 430, 431, 434, 435, 436, 437, 438, 439, 440, 441, 442, 445, 446, 447, 448, 449, 450, 496, 497, 553, 554, 555, 556, 559, 560, 561, 562, 565, 567, 568, 569, 570, 571, 572, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 597, 598, 599, 600, 601, 602, 603, 604, 608, 613, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 686, 687, 716, 717, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIa)

In another aspect, the present invention provides compounds of Formula (VIa)

or pharmaceutically acceptable salts thereof; wherein R¹ and R⁵ are as described herein for Formula (Ia); and n is 0 or 1.

In one embodiment of formula (VIa),

n is 0 or 1;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³ is alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁰, OR¹⁰, Se, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁶)₂, NHC(O)R¹⁶, NR¹⁶C(O)R¹⁶, NHSO₂R¹⁰, NHC(O)OR¹⁶, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, OH, aryl, or heterocyclyl;

R¹⁰ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰, are optionally substituted with one or more independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³ is alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolyl, thienyl, furanyl, cycloalkyl, and cycloalkenyl is optionally substituted with one or more independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴ is alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one or more independently selected OCH₃, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, or cycloalkenyl is optionally substituted with one or more independently selected alkyl, or OCH₃; and

R¹⁵ is alkyl.

In another embodiment of Formula (VIa), n is 0. In another embodiment of Formula (VIa), n is 1. In another embodiment of Formula (VIa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIa), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIa), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIa), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIa), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIa), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIa), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIa), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIa), R¹ is C(O)NH₂. In another embodiment of Formula (VIa), R¹ is F. In another embodiment of Formula (VIa), R¹ is Cl. In another embodiment of Formula (VIa), R¹ is Br. In another embodiment of Formula (VIa), R¹ is CN. In another embodiment of Formula (VIa), R¹ is NH₂. In another embodiment of Formula (VIa), R¹ is NO₂. In another embodiment of Formula (VIa), R¹ is CF₃. In another embodiment of Formula (VIa), R¹ is C(O)OH. In another embodiment of Formula (VIa), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (VIa), which include Examples 285, 286, 287, 288, 289, 290, 426, 427, 437, 445, 553, 554, 555, 556, 599, 627, 628, 629, 630, 631, 632, 633, 634, 635, 686, 687, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (Ib)

One embodiment of this invention, therefore, pertains to compounds or pharmaceutically acceptable salts, which are useful as inhibitors of NAMPT, the compounds having Formula (Ib)

wherein

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R⁴ aryl and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, OR^(B), SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, Se, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁶, NR¹⁶C(O)R¹⁶, NHSO₂R¹⁶, NHC(O)OR¹⁶, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁷, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, NHR¹¹, N(R¹¹)₂, C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, NHSO₂R¹¹, NHC(O)OR¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, NHC(O)NH₂, NHC(O)NHR¹¹, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁸, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁸ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R¹²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹¹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹², at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹² alkyl, alkenyl, and alkynyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (Ib), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (Ib), X¹, X², and X³ are CH. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (Ib), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (Ib), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (Ib), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (Ib), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (Ib), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (Ib), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ib), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), R¹ is C(O)NH₂. In another embodiment of Formula (Ib), R¹ is F. In another embodiment of Formula (Ib), R¹ is Cl. In another embodiment of Formula (Ib), R¹ is Br. In another embodiment of Formula (Ib), R¹ is CN. In another embodiment of Formula (Ib), R¹ is NH₂. In another embodiment of Formula (Ib), R¹ is NO₂. In another embodiment of Formula (Ib), R¹ is CF₃. In another embodiment of Formula (Ib), R¹ is C(O)OH. In another embodiment of Formula (Ib), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ib), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ib), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ib), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In one embodiment of Formula (Ib), R² is phenyl which is substituted at the para position with R⁵; and R⁵ is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one, or isoindolin-1-onyl.

In one embodiment of Formula (Ib),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is alkyl, phenyl, heterocyclyl; wherein each R² alkyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, C(O)R⁴, CO(O)R⁴NHC(O)R⁴, NR⁴C(O)R⁴, C(O)NHR⁴, or C(O)N(R⁴)₂; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, NHS(O)₂R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, SO₂NHR⁵, CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, C(O)R⁵, N(R⁵)₂, NHC(O)R⁵, C(O)NHR⁵, F, Cl, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, OH, F, Cl, Br or I;

R⁴, at each occurrence, is independently selected alkyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl is optionally substituted with one, two, three or four independently selected R⁷, F, Cl, Br or I; wherein each R⁴ aryl cycloalkyl, and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, C(O)R⁸, CO(O)R⁸, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)OR⁹, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl or heterocyclyl; wherein each R⁶ alkyl is optionally substituted with one, two, three or four independently selected F, Cl, Br or I;

R⁷, at each occurrence, is independently selected aryl, or heterocyclyl;

R⁸, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁸ alkyl is optionally substituted with one, two, three or four independently selected R¹², OR¹²OH, CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁹ alkyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹², at each occurrence, is independently selected alkyl, heterocyclyl, or cycloalkyl; wherein each R¹² alkyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹ and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, or cycloalkyl; wherein each R¹³ alkyl and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NHC(O)OR¹⁴, OH, CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, CN, CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, OH, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In another embodiment of Formula (Ib),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is alkyl, phenyl, heterocyclyl; wherein each R² alkyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, C(O)R⁴, CO(O)R⁴NHC(O)R⁴, NR⁴C(O)R⁴, C(O)NHR⁴, or C(O)N(R⁴)₂; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, NHS(O)₂R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, SO₂NHR⁵, or CF₃; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, C(O)R⁵, N(R⁵)₂, NHC(O)R⁵, or C(O)NHR⁵;

R³, at each occurrence, is independently selected alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH;

R⁴, at each occurrence, is independently selected alkyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl is optionally substituted with one, two, three or four independently selected R⁷; wherein each R⁴ aryl cycloalkyl, and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, C(O)R⁸, CO(O)R⁸, F, Cl, or Br;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)OR⁹, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)OH, OH, CN, CF₃, or F;

R⁶, at each occurrence, is independently selected alkyl or heterocyclyl;

R⁷, at each occurrence, is independently selected aryl, or heterocyclyl;

R⁸, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁸ alkyl is optionally substituted with one, two, three or four independently selected R¹², OR¹²OH, or CF₃;

R⁹, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁹ alkyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹², at each occurrence, is independently selected alkyl, heterocyclyl, or cycloalkyl; wherein each R¹² alkyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, or Cl;

R¹³, at each occurrence, is independently selected alkyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, or cycloalkyl; wherein each R¹³ alkyl and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NHC(O)OR¹⁴, OH, or CF₃; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, CN, CF₃, F, or Cl;

R¹⁴, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, or OH; wherein each R¹⁴ aryl, heterocyclyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, or Cl;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

Still another embodiment pertains to compounds having Formula (Ib), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 349, 350, 351, 352, 353, 354, 355, 356, 358, 359, 360, 361, 362, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 451, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 542, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 605, 606, 607, 608, 613, 614, 615, 616, 617, 618, 619, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 655, 656, 657, 658, 659, 660, 661, 662, 663, 664, 665, 666, 667, 668, 669, 670, 671, 672, 673, 674, 675, 676, 677, 678, 679, 680, 681, 682, 683, 684, 685, 686, 687, 688, 689, 690, 691, 692, 693, 694, 695, 696, 697, 698, 699, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, 718, 719, 720, 721, 722, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 754, 755, 756, 757, 758, 759, 760, 761, 762, 763, 764, 765, 766, 767, 768, 769, 770, 771, 772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789, 790, 791, 792, 793, 794, 796, 797, 798, 799, 800, 801, 802, 803, 805, 806, 807, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 839, 840, 841, 842, 843, 844, 845, 846, 847, 848, 849, 850, 851, 852, 853, 854, 855, 856, 857, 858, 859, 860, 861, 862, 863, 864, 865, 866, 867, 868, 869, 870, 871, 872, 873, 874, 875, 876, 877, 878, 879, 880, 881, 882, 883, 884, 885, 886, 887, 888, 889, 890, 891, 892, 893, 894, 895, 896, 897, 898, 899, 900, 901, 902, 903, 904, 905, 906, 907, 908, 909, 910, 911, 912, 913, 914, 915, 916, 917, 918, 919, 920, 921, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931, 932, 933, 934, 935, 936, 937, 938, 939, 940, 941, 942, 943, 944, 945, 946, 947, 948, 949, 950, 951, 952, 953, 954, 955, 956, 957, 958, 959, 960, 961, 962, 963, 964, 965, 966, 967, 968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979, 980, 981, 982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993, 994, 995, 996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007, 1008, 1009, 1010, 1011, 1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1021, 1022, 1023, 1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033, 1034, 1035, 1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045, 1046, 1047, 1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057, 1058, 1059, 1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071, 1072, 1073, 1074, 1075, 1076, 1077, 1078, 1079, 1080, 1081, 1082, 1083, 1084, 1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130, 1131, 1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1159, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1190, 1191, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1200, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1237, 1238, 1239, 1240, 1241, 1242, 1243, 1244, 1245, 1246, 1247, 1248, 1249, 1250, 1251, 1252, 1253, 1254, 1255, 1256, 1257, 1258, 1259, 1260, 1261, 1262, 1263, 1264, 1265, 1266, 1267, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1279, 1280, 1281, 1282, 1283, 1284, 1285, 1286, 1287, 1288, 1289, 1292, 1293, 1294, 1295, 1296, 1297, 1298, 1299, 1300, 1301, 1302, 1303, 1304, 1305, 1306, 1307, 1308, 1309, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 1317, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1337, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1347, 1348, 1349, 1350, 1351, 1352, 1353, 1354, 1355, 1356, 1357, 1358, 1359, 1360, 1361, 1362, 1363, 1364, 1365, 1366, 1367, 1368, 1369, 1370, 1371, 1372, 1373, 1374, 1375, 1376, 1377, 1378, 1379, 1380, 1381, 1382, 1383, 1384, 1385, 1386, 1387, 1388, 1389, 1390, 1391, 1392, 1393, 1394, 1395, 1396, 1397, 1398, 1399, 1400, 1401, 1402, 1403, 1404, 1405, 1406, 1407, 1408, 1409, 1410, 1411, 1412, 1413, 1414, 1415, 1416, 1417, 1418, 1419, 1420, 1421, 1422, 1423, 1424, 1425, 1426, or pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIb)

In another aspect, the present invention provides compounds of Formula (IIb)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (Ib); and R² is phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the R² phenyl, heterocyclyl, cycloalkyl, and cycloalkenyl are optionally substituted as described herein for substituents on R² in Formula (Ib).

In one embodiment of formula (IIb),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, Se, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁶, NR¹⁶C(O)R¹⁶, NHSO₂R¹⁶, NHC(O)OR¹⁶, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (IIb), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IIb), X¹, X², and X³ are CH. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IIb), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IIb), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IIb), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IIb), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IIb), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), R¹ is C(O)NH₂. In another embodiment of Formula (IIb), R¹ is F. In another embodiment of Formula (IIb), R¹ is Cl. In another embodiment of Formula (IIb), R¹ is Br. In another embodiment of Formula (IIb), R¹ is CN. In another embodiment of Formula (IIb), R¹ is NH₂. In another embodiment of Formula (IIb), R¹ is NO₂. In another embodiment of Formula (IIb), R¹ is CF₃. In another embodiment of Formula (IIb), R¹ is C(O)OH. In another embodiment of Formula (IIb), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Bb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (IIb), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 325, 326, 327, 328, 329, 330, 331, 332, 333, 334, 335, 336, 337, 338, 339, 340, 341, 342, 343, 344, 345, 346, 347, 348, 368, 369, 370, 371, 372, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 404, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 422, 423, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 452, 453, 454, 455, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 495, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 550, 551, 552, 553, 554, 555, 556, 557, 558, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 574, 575, 576, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 614, 615, 617, 618, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 648, 649, 650, 651, 652, 653, 654, 682, 683, 684, 685, 686, 687, 700, 701, 702, 703, 704, 705, 706, 707, 708, 709, 710, 711, 712, 713, 714, 715, 716, 717, 718, 719, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 754, 755, 756, 758, 759, 760, 761, 762, 763, 764, 765, 766, 767, 768, 769, 770, 771, 772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789, 790, 791, 792, 793, 794, 796, 799, 800, 801, 802, 803, 805, 806, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 839, 840, 841, 842, 843, 844, 845, 846, 847, 848, 849, 850, 851, 852, 853, 854, 855, 856, 857, 858, 859, 860, 861, 862, 863, 864, 865, 866, 867, 868, 869, 870, 871, 873, 874, 875, 876, 877, 878, 879, 880, 881, 882, 883, 884, 885, 886, 887, 888, 889, 890, 891, 892, 893, 894, 895, 896, 897, 898, 899, 900, 901, 902, 903, 904, 905, 906, 907, 908, 910, 911, 912, 913, 914, 915, 916, 917, 918, 919, 920, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931, 932, 933, 934, 935, 936, 937, 938, 939, 940, 941, 942, 943, 944, 945, 946, 947, 948, 949, 950, 951, 952, 953, 954, 955, 956, 957, 958, 959, 960, 961, 962, 963, 964, 965, 966, 967, 968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979, 980, 981, 982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993, 994, 995, 996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007, 1008, 1009, 1010, 1011, 1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1021, 1022, 1023, 1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033, 1034, 1035, 1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045, 1046, 1047, 1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057, 1058, 1059, 1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071, 1072, 1073, 1074, 1075, 1076, 1077, 1078, 1079, 1080, 1081, 1082, 1083, 1084, 1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130, 1131, 1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1159, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1190, 1191, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1200, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1237, 1238, 1239, 1240, 1241, 1242, 1243, 1244, 1245, 1246, 1247, 1248, 1249, 1250, 1251, 1252, 1253, 1254, 1255, 1256, 1257, 1258, 1259, 1260, 1261, 1262, 1263, 1264, 1265, 1266, 1267, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1279, 1280, 1281, 1282, 1283, 1284, 1288, 1289, 1292, 1293, 1294, 1295, 1296, 1297, 1298, 1299, 1300, 1301, 1302, 1303, 1304, 1305, 1306, 1307, 1308, 1309, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 1317, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1337, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1347, 1348, 1349, 1363, 1364, 1365, 1366, 1367, 1368, 1370, 1371, 1372, 1373, 1374, 1375, 1376, 1377, 1378, 1379, 1380, 1381, 1382, 1383, 1384, 1385, 1386, 1387, 1388, 1389, 1390, 1391, 1392, 1393, 1394, 1395, 1396, 1397, 1398, 1399, 1400, 1401, 1402, 1403, 1404, 1405, 1406, 1407, 1408, 1409, 1410, 1411, 1412, 1413, 1414, 1415, 1416, 1417, 1418, 1419, 1420, 1421, 1422, 1423, 1424, 1425, 1426, or pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIIb)

In another aspect, the present invention provides compounds of Formula (IIIb)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (Ib); and R^(X) is as described herein for substituents at the para position in Formula (Ib) when R² is phenyl.

In one embodiment of formula (Mb),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R^(x) is R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁹ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when X¹, X², and X³ are CH; R^(x) is not methyl;

with the proviso that when X¹, X², and X³ are CH; R^(x) is not methoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (IIIb), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IIIb), X¹, X², and X³ are CH. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IIIb), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IIIb), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IIIb), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IIIb), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IIIb), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IIIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), R¹ is C(O)NH₂. In another embodiment of Formula (IIIb), R¹ is F. In another embodiment of Formula (IIIb), R¹ is Cl. In another embodiment of Formula (IIIb), R¹ is Br. In another embodiment of Formula (IIIb), R¹ is CN. In another embodiment of Formula (IIIb), R¹ is NH₂. In another embodiment of Formula (IIIb), R¹ is NO₂. In another embodiment of Formula (IIIb), R¹ is CF₃. In another embodiment of Formula (IIIb), R¹ is C(O)OH. In another embodiment of Formula (IIIb), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In one embodiment of formula (TIN, R^(x) is R⁵, OR⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, NHS(O)₂R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, SO₂NHR⁵ or CF₃. In another embodiment of formula (IIIb), R^(x) is R⁵, and R⁵ is heterocyclyl, which is optionally substituted as described in embodiments herein.

In another embodiment of Formula (IIIb), R^(x) is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one, isoindolin-1-onyl, or 1,2,3,6-tetrahydropyridinyl. In another embodiment of Formula (IIIb), R^(x) is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, isoindolin-1-onyl, or pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one; which are optionally substituted as defined herein. In another embodiment of Formula (IIIb), R^(x) is, 2,3,6-tetrahydropyridinyl; which is optionally substituted as defined herein.

Still another embodiment pertains to compounds having Formula (IIIb), which include Examples 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84, 85, 86, 87, 88, 89, 90, 91, 92, 93, 94, 95, 96, 97, 98, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 158, 159, 160, 161, 162, 163, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 175, 176, 177, 178, 179, 180, 181, 182, 183, 184, 185, 186, 187, 188, 189, 190, 191, 192, 193, 194, 195, 196, 197, 198, 199, 200, 201, 202, 203, 204, 205, 206, 207, 208, 209, 210, 211, 212, 213, 214, 215, 216, 217, 218, 219, 220, 221, 222, 223, 224, 225, 226, 227, 228, 229, 230, 231, 232, 233, 234, 235, 236, 237, 238, 239, 240, 241, 242, 243, 244, 245, 246, 247, 248, 249, 250, 251, 252, 253, 254, 255, 256, 257, 258, 259, 260, 261, 262, 263, 264, 265, 266, 267, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 287, 288, 289, 290, 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 316, 317, 318, 319, 320, 321, 322, 323, 324, 327, 330, 331, 332, 333, 336, 337, 338, 339, 340, 341, 342, 343, 348, 373, 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 401, 402, 403, 405, 406, 407, 408, 409, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 425, 426, 427, 428, 429, 430, 431, 432, 433, 434, 435, 436, 437, 438, 439, 440, 441, 442, 443, 444, 445, 446, 447, 448, 449, 450, 456, 457, 458, 459, 460, 461, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 479, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 496, 497, 498, 499, 500, 501, 502, 503, 504, 505, 506, 507, 508, 509, 510, 511, 512, 513, 514, 515, 516, 517, 518, 519, 520, 521, 522, 523, 524, 525, 526, 527, 528, 529, 530, 531, 532, 533, 534, 535, 536, 537, 538, 539, 540, 541, 543, 544, 545, 546, 547, 548, 549, 553, 554, 555, 556, 559, 560, 561, 562, 563, 564, 565, 566, 567, 568, 569, 570, 571, 572, 573, 577, 578, 579, 580, 581, 582, 583, 584, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 596, 597, 598, 599, 600, 601, 602, 603, 604, 607, 608, 613, 620, 621, 622, 623, 624, 625, 626, 627, 628, 629, 630, 631, 632, 633, 634, 635, 636, 637, 638, 639, 640, 641, 642, 643, 644, 645, 646, 647, 649, 650, 682, 683, 684, 685, 686, 687, 705, 706, 707, 708, 709, 710, 716, 717, 718, 719, 723, 724, 725, 726, 727, 728, 729, 730, 731, 732, 733, 734, 735, 736, 737, 738, 739, 740, 741, 742, 743, 744, 745, 746, 747, 748, 749, 750, 751, 752, 753, 754, 755, 756, 759, 760, 761, 762, 763, 770, 771, 772, 773, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 787, 788, 789, 790, 791, 792, 793, 794, 796, 799, 802, 803, 806, 808, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 824, 825, 826, 827, 828, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 840, 841, 842, 843, 844, 845, 846, 847, 848, 849, 850, 851, 852, 853, 854, 855, 856, 857, 858, 859, 860, 861, 862, 863, 864, 865, 866, 867, 868, 869, 870, 871, 873, 874, 875, 876, 877, 878, 879, 880, 881, 882, 883, 884, 885, 886, 887, 888, 889, 890, 891, 892, 893, 894, 895, 896, 897, 898, 899, 900, 901, 902, 903, 904, 905, 906, 907, 908, 910, 911, 912, 913, 914, 915, 916, 917, 918, 919, 922, 923, 924, 925, 926, 927, 928, 929, 930, 931, 932, 933, 934, 935, 936, 937, 938, 939, 940, 941, 942, 943, 944, 945, 946, 947, 948, 949, 950, 951, 952, 966, 967, 968, 969, 970, 971, 972, 973, 974, 975, 976, 977, 978, 979, 980, 981, 982, 983, 984, 985, 986, 987, 988, 989, 990, 991, 992, 993, 994, 995, 996, 997, 998, 999, 1000, 1001, 1002, 1003, 1004, 1005, 1006, 1007, 1008, 1009, 1010, 1011, 1012, 1013, 1014, 1015, 1016, 1017, 1018, 1019, 1021, 1022, 1023, 1024, 1025, 1026, 1027, 1028, 1029, 1030, 1031, 1032, 1033, 1034, 1035, 1036, 1037, 1038, 1039, 1040, 1041, 1042, 1043, 1044, 1045, 1046, 1047, 1048, 1049, 1050, 1051, 1052, 1053, 1054, 1055, 1056, 1057, 1058, 1059, 1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071, 1072, 1073, 1074, 1075, 1076, 1077, 1078, 1079, 1080, 1081, 1082, 1083, 1084, 1085, 1086, 1087, 1088, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1099, 1100, 1101, 1102, 1103, 1104, 1105, 1106, 1107, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1126, 1127, 1128, 1129, 1130, 1131, 1132, 1133, 1134, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1151, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1159, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1190, 1191, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1200, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1237, 1238, 1239, 1240, 1241, 1242, 1243, 1244, 1245, 1246, 1247, 1248, 1249, 1250, 1251, 1252, 1253, 1254, 1255, 1256, 1257, 1258, 1259, 1260, 1261, 1262, 1263, 1264, 1265, 1266, 1267, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1279, 1280, 1281, 1282, 1283, 1284, 1288, 1289, 1292, 1293, 1294, 1295, 1296, 1297, 1298, 1299, 1300, 1301, 1302, 1303, 1304, 1305, 1306, 1307, 1308, 1309, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 1317, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1337, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1347, 1348, 1349, 1363, 1364, 1365, 1366, 1367, 1368, 1370, 1371, 1372, 1373, 1374, 1375, 1376, 1377, 1378, 1379, 1380, 1381, 1382, 1383, 1384, 1385, 1386, 1387, 1388, 1389, 1390, 1391, 1392, 1393, 1394, 1395, 1396, 1397, 1398, 1399, 1400, 1401, 1402, 1403, 1404, 1405, 1406, 1407, 1408, 1409, 1410, 1411, 1412, 1413, 1414, 1415, 1416, 1417, 1418, 1419, 1420, 1421, 1422, 1423, 1424, 1425, 1426, or pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds having Formula (IIIb), which include 374, 375, 376, 377, 378, 379, 380, 381, 382, 383, 384, 385, 386, 387, 388, 389, 390, 391, 392, 393, 394, 395, 396, 397, 398, 399, 400, 547, 548, 549, 550, 551, 552, and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IVb)

In another aspect, the present invention provides compounds of Formula (IVb)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (Ib).

In one embodiment of formula (IVb),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (IVb), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IVb), X¹, X², and X³ are CH. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IVb), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IVb), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IVb), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IVb), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IVb), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IVb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), R¹ is C(O)NH₂. In another embodiment of Formula (IVb), R¹ is F. In another embodiment of Formula (IVb), R¹ is Cl. In another embodiment of Formula (IVb), R¹ is Br. In another embodiment of Formula (IVb), R¹ is CN. In another embodiment of Formula (IVb), R¹ is NH₂. In another embodiment of Formula (IVb), R¹ is NO₂. In another embodiment of Formula (IVb), R¹ is CF₃. In another embodiment of Formula (IVb), R¹ is C(O)OH. In another embodiment of Formula (IVb), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (IVb), which include Examples 291, 292, 293, 294, 295, 296, 297, 298, 299, 300, 301, 302, 303, 304, 305, 306, 307, 308, 309, 310, 311, 312, 313, 314, 315, 563, 564, 577, 579, 580, 581, 582, 583, 584, 596, 607, 649, 650, 682, 683, 684, 685, 789, 791, 792, 793, 794, 796, 874, 878, 879, 919, 932, 934, 935, 1363, 1364, 1365, 1366, 1367, 1368, 1370, 1371, 1372, or pharmaceutically acceptable salts thereof.

Embodiments of Formula (Vb)

In another aspect, the present invention provides compounds of Formula (Vb)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (Ib).

In one embodiment of formula (Vb),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (Vb), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (Vb), X¹, X², and X³ are CH. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (Vb), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (Vb), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (Vb), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (Vb), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (Vb), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (Vb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), R¹ is C(O)NH₂. In another embodiment of Formula (Vb), R¹ is F. In another embodiment of Formula (Vb), R¹ is Cl. In another embodiment of Formula (Vb), R¹ is Br. In another embodiment of Formula (Vb), R¹ is CN. In another embodiment of Formula (Vb), R¹ is NH₂. In another embodiment of Formula (Vb), R¹ is NO₂. In another embodiment of Formula (Vb), R¹ is CF₃. In another embodiment of Formula (Vb), R¹ is C(O)OH. In another embodiment of Formula (Vb), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Vb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Vb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Vb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (Vb), which include Examples 1, 2, 3, 4, 5, 8, 9, 10, 13, 14, 16, 17, 18, 20, 21, 23, 24, 25, 26, 28, 29, 30, 31, 32, 33, 34, 36, 37, 38, 39, 40, 42, 43, 45, 46, 48, 49, 53, 54, 57, 58, 59, 60, 61, 62, 63, 66, 67, 68, 70, 71, 73, 75, 77, 79, 80, 81, 82, 83, 85, 86, 87, 88, 90, 91, 92, 93, 94, 95, 97, 98, 99, 100, 101, 103, 104, 105, 106, 107, 108, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 139, 140, 141, 142, 143, 144, 145, 146, 148, 149, 150, 151, 152, 153, 154, 155, 156, 157, 159, 164, 165, 166, 167, 168, 169, 170, 171, 172, 173, 174, 176, 177, 178, 179, 180, 181, 182, 184, 188, 189, 190, 192, 193, 194, 196, 199, 201, 203, 204, 205, 209, 210, 211, 213, 215, 217, 220, 223, 224, 226, 227, 228, 230, 231, 232, 234, 235, 236, 237, 239, 243, 245, 252, 253, 256, 258, 260, 268, 269, 270, 271, 272, 273, 274, 275, 276, 277, 278, 279, 280, 281, 282, 283, 284, 285, 286, 288, 289, 290, 373, 410, 411, 412, 413, 414, 415, 416, 417, 418, 419, 420, 421, 424, 426, 427, 430, 431, 435, 436, 437, 440, 441, 442, 445, 446, 447, 449, 450, 496, 497, 553, 554, 555, 556, 559, 560, 562, 567, 568, 569, 570, 571, 572, 585, 586, 587, 588, 589, 590, 591, 592, 593, 594, 595, 597, 598, 599, 600, 601, 602, 603, 604, 608, 613, 625, 626, 628, 629, 630, 631, 632, 633, 634, 687, 716, 717, 718, 719, 723, 728, 729, 731, 732, 733, 734, 735, 737, 738, 739, 741, 743, 744, 745, 747, 748, 752, 770, 771, 774, 775, 776, 777, 778, 779, 780, 781, 782, 783, 784, 785, 786, 790, 802, 803, 809, 810, 811, 812, 813, 814, 815, 816, 817, 818, 819, 820, 821, 822, 823, 826, 827, 829, 830, 831, 832, 833, 834, 835, 836, 837, 838, 856, 857, 858, 875, 880, 881, 882, 884, 894, 895, 922, 923, 924, 925, 939, 969, 970, 971, 972, 976, 977, 978, 1063, 1064, 1065, 1089, 1090, 1091, 1092, 1093, 1094, 1095, 1096, 1097, 1098, 1100, 1102, 1103, 1104, 1105, 1106, 1108, 1109, 1110, 1111, 1112, 1113, 1114, 1115, 1116, 1117, 1118, 1119, 1120, 1121, 1122, 1123, 1124, 1125, 1127, 1129, 1130, 1132, 1133, 1135, 1136, 1137, 1138, 1139, 1140, 1141, 1142, 1143, 1144, 1145, 1146, 1147, 1148, 1149, 1150, 1152, 1153, 1154, 1155, 1156, 1157, 1158, 1160, 1161, 1162, 1163, 1164, 1165, 1166, 1167, 1168, 1169, 1170, 1171, 1172, 1173, 1174, 1175, 1176, 1177, 1178, 1179, 1180, 1181, 1182, 1183, 1184, 1185, 1186, 1187, 1188, 1189, 1192, 1193, 1194, 1195, 1196, 1197, 1198, 1199, 1201, 1202, 1203, 1204, 1205, 1206, 1207, 1208, 1209, 1210, 1211, 1212, 1213, 1214, 1215, 1216, 1217, 1218, 1219, 1220, 1221, 1222, 1223, 1224, 1225, 1226, 1227, 1228, 1229, 1230, 1231, 1232, 1233, 1234, 1235, 1236, 1239, 1240, 1241, 1242, 1243, 1245, 1260, 1261, 1262, 1263, 1264, 1266, 1267, 1268, 1269, 1270, 1271, 1272, 1273, 1274, 1275, 1276, 1277, 1278, 1310, 1311, 1312, 1313, 1314, 1315, 1316, 1317, 1318, 1319, 1320, 1321, 1322, 1323, 1324, 1325, 1326, 1327, 1328, 1329, 1330, 1331, 1332, 1333, 1334, 1335, 1336, 1337, 1338, 1339, 1340, 1341, 1342, 1343, 1344, 1345, 1346, 1348, 1349, or pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIb)

In another aspect, the present invention provides compounds of Formula (VIb)

or pharmaceutically acceptable salts thereof; wherein R¹ and R⁵ are as described herein for Formula (Ia); and n is 0 or 1.

In one embodiment of formula (VIb),

n is 0 or 1;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.

In another embodiment of Formula (VIb), n is 0. In another embodiment of Formula (VIb), n is 1. In another embodiment of Formula (VIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIb), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIb), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIb), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIb), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIb), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIb), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIb), R¹ is C(O)NH₂. In another embodiment of Formula (VIb), R¹ is F. In another embodiment of Formula (VIb), R¹ is Cl. In another embodiment of Formula (VIb), R¹ is Br. In another embodiment of Formula (VIb), R¹ is CN. In another embodiment of Formula (VIb), R¹ is NH₂. In another embodiment of Formula (VIb), R¹ is NO₂. In another embodiment of Formula (VIb), R¹ is CF₃. In another embodiment of Formula (VIb), R¹ is C(O)OH. In another embodiment of Formula (VIb), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (VIb), which include Examples 285, 286, 288, 289, 290, 426, 427, 437, 445, 553, 554, 555, 556, 599, 627, 628, 629, 630, 631, 632, 633, 634, 635, 686, 687, 718, 723, 725, 726, 727, 728, 729, 731, 732, 733, 734, 735, 737, 738, 739, 741, 743, 744, 745, 747, 748, 749, 750, 751, 752, 770, 771, 773, 774, 775, 776, 777, 778, 779, 780, 803, 875, 880, 881, 882, 884, 922, 923, 924, 925, 939, 969, 970, 971, 972, 1055, 1056, 1057, 1058, 1059, 1060, 1061, 1062, 1063, 1064, 1065, 1066, 1067, 1068, 1069, 1070, 1071, 1072, 1073, 1074, 1075, 1076, or pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIIb)

In another aspect, the present invention provides compounds of Formula (VIIb)

or pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R¹³ are as described herein for Formula (Ib), and

indicates a single or a double bond.

In one embodiment of formula (VIIb),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁶, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (VIIb), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (VIIb), X¹, X², and X³ are CH. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (VIIb), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (VIIb), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (VIIb), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (VIIb), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (VIIb), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (VIIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIb), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), R¹ is C(O)NH₂. In another embodiment of Formula (VIIb), R¹ is F. In another embodiment of Formula (VIIb), R¹ is Cl. In another embodiment of Formula (VIIb), R¹ is Br. In another embodiment of Formula (VIIb), R¹ is CN. In another embodiment of Formula (VIIb), R¹ is NH₂. In another embodiment of Formula (VIIb), R¹ is NO₂. In another embodiment of Formula (VIIb), R¹ is CF₃. In another embodiment of Formula (VIIb), R¹ is C(O)OH. In another embodiment of Formula (VIIb), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIb), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIb), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIb), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (VIIb), which include Examples 317, 330, 331, 332, 401, 405, 406, 407, 432, 456, 457, 458, 459, 460, 462, 463, 464, 465, 466, 467, 468, 469, 470, 471, 472, 473, 474, 475, 476, 477, 478, 480, 481, 482, 483, 484, 485, 486, 487, 488, 489, 490, 491, 492, 493, 494, 543, 544, 545, 546, 620, 646, 647, 705, 706, 707, 708, 709, 710, 759, 760, 761, 762, 763, 799, 910, 911, 912, 913, 914, 915, 916, 917, 918, 967, 968, 979, 980, 981, 982, 983, 984, 985, 986, 1014, 1015, 1016, 1017, 1019, 1077, 1078, 1079, 1080, 1254, 1255, 1256, 1257, 1258, 1259, 1279, 1280, 1281, 1282, 1283, 1284, 1384, 1385, or pharmaceutically acceptable salts thereof.

Embodiments of Formula (Ic)

One embodiment of this invention, therefore, pertains to compounds or pharmaceutically acceptable salts, which are useful as inhibitors of NAMPT, the compounds having Formula (Ic)

wherein

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R⁴ aryl and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, OR^(B), SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁷, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, NHR¹¹, N(R¹¹)₂, C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, NHSO₂R¹¹, NHC(O)OR¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, NHC(O)NH₂, NHC(O)NHR¹¹, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁸, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁸ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R¹²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹¹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹², at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹² alkyl, alkenyl, and alkynyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁹, R¹¹, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I; wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy;

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (Ic), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (Ic), X¹, X², and X³ are CH. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (Ic), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (Ic), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (Ic), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (Ic), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (Ic), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (Ic), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ic), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), R¹ is C(O)NH₂. In another embodiment of Formula (Ic), R¹ is F. In another embodiment of Formula (Ic), R¹ is Cl. In another embodiment of Formula (Ic), R¹ is Br. In another embodiment of Formula (Ic), R¹ is CN. In another embodiment of Formula (Ic), R¹ is NH₂. In another embodiment of Formula (Ic), R¹ is NO₂. In another embodiment of Formula (Ic), R¹ is CF₃. In another embodiment of Formula (Ic), R¹ is C(O)OH. In another embodiment of Formula (Ic), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ic), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ic), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Ic), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In one embodiment of Formula (Ic), R² is phenyl which is substituted at the para position with R⁵; and R⁵ is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one, or isoindolin-1-onyl.

In one embodiment of Formula (Ic),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is alkyl, phenyl, cycloalkyl, or heterocyclyl; wherein each R² alkyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, C(O)R⁴, CO(O)R⁴NHC(O)R⁴, NR⁴C(O)R⁴, C(O)NHR⁴, or C(O)N(R⁴)₂; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, NHS(O)₂R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, SO₂NHR⁵, CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl and cycloalkyl are optionally substituted with one, two, three or four independently selected R⁵, OR⁵, C(O)R⁵, C(O)OR⁵, N(R⁵)₂, NHC(O)R⁵, C(O)NHR⁵, F, Cl, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, OH, F, Cl, Br or I;

R⁴, at each occurrence, is independently selected alkyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl is optionally substituted with one, two, three or four independently selected R⁷, F, Cl, Br or I; wherein each R⁴ aryl cycloalkyl, and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, C(O)R⁸, CO(O)R⁸, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)OR⁹, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)OH, OH, CN, CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl or heterocyclyl; wherein each R⁶ alkyl is optionally substituted with one, two, three or four independently selected F, Cl, Br or I;

R⁷, at each occurrence, is independently selected aryl, or heterocyclyl;

R⁸, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁸ alkyl is optionally substituted with one, two, three or four independently selected R¹², OR¹²OH, CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁹ alkyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹², at each occurrence, is independently selected alkyl, heterocyclyl, or cycloalkyl; wherein each R¹² alkyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹ and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SO₂R¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NHC(O)OR¹⁴, OH, CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, OH, CN, CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, OH, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In another embodiment of Formula (Ic),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R² is alkyl, phenyl, cycloalkyl, or heterocyclyl; wherein each R² alkyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, C(O)R⁴, CO(O)R⁴NHC(O)R⁴, NR⁴C(O)R⁴, C(O)NHR⁴, or C(O)N(R⁴)₂; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, NHS(O)₂R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, SO₂NHR⁵, or CF₃; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl and cycloalkyl are optionally substituted with one, two, three or four independently selected R⁵, OR⁵, C(O)R⁵, C(O)OR⁵, N(R⁵)₂, NHC(O)R⁵, or C(O)NHR⁵;

R³, at each occurrence, is independently selected alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH;

R⁴, at each occurrence, is independently selected alkyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl is optionally substituted with one, two, three or four independently selected R⁷; wherein each R⁴ aryl cycloalkyl, and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, C(O)R⁸, CO(O)R⁸, F, Cl, or Br;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, C(O)R⁹, NH₂, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)OR⁹, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)OH, OH, CN, CF₃, or F;

R⁶, at each occurrence, is independently selected alkyl or heterocyclyl;

R⁷, at each occurrence, is independently selected aryl, or heterocyclyl;

R⁸, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁸ alkyl is optionally substituted with one, two, three or four independently selected R¹², OR¹²OH, or CF₃;

R⁹, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁹ alkyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹², at each occurrence, is independently selected alkyl, heterocyclyl, or cycloalkyl; wherein each R¹² alkyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, or Cl;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SO₂R¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NHC(O)OR¹⁴, OH, or CF₃; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, CN, OH, CF₃, F, or Cl;

R¹⁴, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, or OH; wherein each R¹⁴ aryl, heterocyclyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, or Cl;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

Still another embodiment pertains to compounds having Formula (Ic), which include

-   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(furo[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(thieno[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dihydro-1,4-benzodioxin-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-fluoro-5-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-acetylphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,3-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(6-aminohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-benzodioxol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dihydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-propoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-2-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methyl-1H-indazol-5-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     5-({4[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}amino)-1H-indazole-3-carboxylate; -   N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(5-chloropyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-fluorobenzoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methoxy-1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-propoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(dimethylamino)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoro-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1,3-benzodioxol-5-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-{4-[(2-phenoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-hydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({1-[(3S)-tetrahydrofuran-3-yl]-1H-pyrazol-4-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,4-dioxa-8-azaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylthio)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(trifluoromethyl)thio]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-fluorophenyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(hydroxymethyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-benzodioxol-5-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-isopropyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiomorpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzylpiperidin-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-acetamido-2-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[3-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-imidazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-(3-cyanophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(2-hydroxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyanomethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclohexylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1H-indol-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(phenylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(diethylamino)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-phenylethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-aminophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     (1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}piperidin-4-yl)carbamate; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(cyclohexylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-chlorobenzyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(diethylcarbamoyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-hydroxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-6-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-fluoropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylmethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3,4,9-tetrahydro-2H-beta-carbolin-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tert-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[4-(trifluoromethyl)phenyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-difluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-benzylpyrrolidin-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-carbamoylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopropylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(methylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dioxolan-2-ylmethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(4-fluorophenyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-phenyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(sec-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(ethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isobutyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(trifluoromethyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,6-dimethylmorpholin-4-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(prop-2-yn-1-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyanoethyl)(cyclopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(isopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-N-isopropyl-beta-alanine; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5,6-dimethoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-chlorophenoxy)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate; -   2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic     acid; -   5-amino-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(aminomethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(2-hydroxy-2-methylpropanoyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetamido-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(N,N-dimethylglycyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methoxyacetyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methylsulfonyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4,4,4-trifluorobutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpentanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(benzyloxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[N-(2-furoyl)glycyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-thienyl)butanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-oxo-4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(N-benzoylglycyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenoxybutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propionylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(heptanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pent-4-enoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-methylpiperazin-1-yl)propanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate; -   2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic     acid; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyclopentylethyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate; -   N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1E)-5-phenylpent-1-en-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[6-(1-propyl-1H-pyrazol-4-yl)pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[1-(3-methylbutyl)-1H-pyrazol-4-yl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-phenylpentyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[2-fluoro-4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{2-fluoro-4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(isopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1     ‘-isobutyryl-1’,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1     ‘-benzoyl-1’,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(isopropylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(benzoylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(butyrylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperazine-1-carboxylate; -   N-[4-(4-propionylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopropylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-butyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-isobutyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-benzoyl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[2-(3-methylbutyl)-2,3-dihydro-1H-isoindol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexyloxy)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[6-(4-chlorophenoxy)hexyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(piperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N,N′-hexane-1,6-diylbis(1,3-dihydro-2H-isoindole-2-carboxamide); -   N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide; ethyl     6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoate; -   N-hexyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-octyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(1-methyl-1H-pyrazol-4-yl)amino]-6-oxohexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[6-(methylamino)-6-oxohexyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-oxo-6-[(3-phenylpropyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-methylbutyl)amino]-6-oxohexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(5-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-phenylpropyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-phenylpropyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(8-fluoro-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(morpholin-4-ylmethyl)-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-4,5-dihydro-3H-2,3-benzodiazepin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(1-methylpiperidin-4-yl)oxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3R)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3S)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(azetidin-1-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperidine-1-carboxylate; -   N-[4-(5-propyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[5-(3-methylbutyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-benzyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-chloropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-oxopyrrolidin-1-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-hydroxycyclopropyl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]-1H-benzimidazol-2-yl}piperazine-1-carboxylate; -   N-[2-(piperazin-1-yl)-1H-benzimidazol-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-vinyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-benzoylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(tetrahydrofuran-3-yl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-(4-{[(3-phenylpropyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-{4-[1-(4-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(tetrahydrofuran-3-ylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2S)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2R)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-phenylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-methoxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-4-yl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-(2-methoxyethyl)-N²-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-(4-cyanophenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(trifluoromethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(tetrahydrofuran-3-ylmethyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(1,2-dihydroxyethyl)-N-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-butyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide;     and -   N-[2-(4-acetylpiperazin-1-yl)-1H-benzimidazol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-D-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propionyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-chlorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-furoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-thienylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrrol-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2,5-dimethyl-1H-pyrrol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,3-thiazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isonicotinoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridazin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrimidin-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(piperidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[6-(benzoylamino)hexyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(benzoylamino)methyl]benzyl}carbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-L-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-D-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(1-acetylpiperidin-4-yl)carbonyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-acetamidobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(methylsulfonyl)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-butyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isobutyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methylbutanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,3,3-trifluoropropanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(methoxyacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopentylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclohexylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[3-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,4-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,5-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(3,4-dimethoxyphenyl)acetyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrrol-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrazol-5-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isonicotinoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridazin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrazin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrimidin-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(N,N-dimethyl-beta-alanyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-acetylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1,3-thiazol-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(morpholin-4-ylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1-(2-phenylethyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-[2-(dimethylamino)ethyl]-N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(morpholin-4-ylcarbonyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{benzyl[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutoxycarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     4-{[(5-cyano-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoate; -   N-(4-{(E)-[(benzyloxy)imino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-aminopyrrolidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-methylbutyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-phenylpropyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-[4-({benzyl[3-(morpholin-4-yl)propyl]amino}methyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-methyl-1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-methoxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-hydroxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(aminomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-(methylthio)butan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3S)-1-hydroxy-3-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3R)-1,3-dihydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxyhexan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2R)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-cyclohexyl-3-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({(2R)-1-hydroxy-3-[(4-methylbenzyl)thio]propan-2-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-tert-butylphenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methoxy-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide;     N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[6-(benzoylamino)hexyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(2-methoxyethoxy)acetyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]pyrazin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-acetamidohexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(1E)-3-[benzyl(methyl)amino]prop-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-phenoxypiperidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-phenoxyazetidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[benzyl(methyl)amino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[2-(2-oxopyrrolidin-1-yl)ethyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1-benzylpiperidin-4-yl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(morpholin-4-yl)benzyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxypropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-3-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{1′-[(2-methoxyethoxy)acetyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[4-(methylsulfonyl)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(ethoxyacetyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(cyclopentylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-hydroxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-hydroxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-hydroxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-methoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-methoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-methoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-fluorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-fluorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-fluorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2-chlorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-chlorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-chlorobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-cyanobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(4-cyanobenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[3-(dimethylamino)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[4-(dimethylamino)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[3-(trifluoromethyl)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[4-(trifluoromethyl)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[3-(trifluoromethoxy)benzoyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2,3-dimethoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2,4-dimethoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(2,5-dimethoxybenzoyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(phenylacetyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(3-fluorophenyl)acetyl]amino}hexyl)-1,3-dihydro-2H-isoindole-2-carboxamide;

5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide;

-   N-{4-[(ethoxyacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(morpholin-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[6-(benzoylamino)hexyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   4-fluoro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-cyano-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-{6-[(pyridin-3-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(pyridin-2-ylcarbonyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1-methylpyrrolidin-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(7-oxo-7-{[(3R)-tetrahydrofuran-3-ylmethyl]amino}heptyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{7-oxo-7-[(tetrahydro-2H-pyran-4-ylmethyl)amino]heptyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(azetidin-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(morpholin-4-ylmethyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methylpiperazin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(3-methylbutyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-hydroxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-chlorobenzoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1-methylpyrrolidin-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-aminoethyl)-1H-imidazol-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2,2-dimethyl-1,3-dioxolan-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-methoxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}-2-oxoethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-{benzyl[3-(morpholin-4-yl)propyl]amino}-3-oxopropyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(6-bromo-2-oxoquinolin-1(2H)-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[6-(3-acetylphenyl)-2-oxoquinolin-1(2H)-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(morpholin-4-ylacetyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(morpholin-4-ylacetyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazol-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2-benzyl-1,3-thiazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(7-{benzyl[3-(morpholin-4-yl)propyl]amino}-7-oxoheptyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-thiazol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(4-methylphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-dihydroxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(ethylsulfonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2,3-dihydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1-hydroxy-4-methylpentan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(5-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.3]hept-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.4]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,9-diazaspiro[5.5]undec-3-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5     (3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5     (3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{benzyl[3-(morpholin-4-yl)propyl]amino}-4-oxobutyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-phenylbutyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetyl-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-hydroxyethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butyrylamino)phenyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methoxybenzyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(2-oxa-7-azaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[6-(3-acetylphenyl)-4-(3-hydroxypropyl)-2-oxoquinolin-1(2H)-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-(acetamidomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[2-(2-chlorobenzyl)-1,3-thiazol-4-yl]-2-thienyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-fluorophenyl)butyl]-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(2-hydroxypropan-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     {4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzyl}carbamate; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(methoxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(tetrahydrofuran-2-ylmethyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methoxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[4-(2-methoxyethyl)piperazin-1-yl]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-pentanoylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butyrylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(1-acetylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(1-isobutyrylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(3-methylbutanoyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(methoxyacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     (2-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}ethyl)carbamate; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-phenylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxyphenyl)acetyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-benzoylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-ethoxypropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl[(1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}azetidin-3-yl)methyl]carbamate; -   N-(4-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(morpholin-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2-methoxyethoxy)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(2,3-dimethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxycyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[4-(acetylamino)phenyl]sulfonyl}amino)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(propylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-propylphenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(butylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[({[(1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methyl}sulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(benzylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-fluorophenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(thiophen-2-ylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(N,N-dimethylglycyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(4,4-difluorocyclohexyl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-(4-{[1-(1,3-thiazol-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide;

5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;

5-fluoro-N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;

-   5-fluoro-N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-D-phenylalaninamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(5-methyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-carbamoylbenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   Nalpha-{4-[(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(4,5,6,7-tetrahydro-1H-indazol-5-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   5-fluoro-N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanocyclopropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   methyl     1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate; -   N-(4-{3-[(3-methylbutyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydrofuran-2-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(benzylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(cyclopentylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(cyclopentylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(2-methoxyethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrrolidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[(dimethylamino)methyl]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-oxazol-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorobenzyl)(3-methylbutanoyl)amino]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[7-chloro-1-(2-hydroxyethyl)-3-oxo-1,3-dihydrocyclobuta[c]quinolin-4(2H)-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butanoylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-difluoroethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[2(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiophen-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pyrimidin-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-acetylpiperidin-4-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{7-oxo-7-[(3-phenylpropyl)amino]heptyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1,3-thiazol-5-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-oxo-4,5,6,7-tetrahydro-1-benzofuran-3-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{2-[(3-methylbutanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(4-methylpentanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(ethoxyacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{[(2-methoxyethoxy)acetyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-2-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[2-(benzoylamino)ethyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-3-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-propanoylazetidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(p     ent-4-ynoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethylglycyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethyl-beta-alanyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrrolidin-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(pyrrolidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methylpiperazin-1-yl)acetyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopropylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopentylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(butylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-fluorophenyl)sulfonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propan-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(benzylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4,4-difluoro     cyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-D-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpentanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridazin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrimidin-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   benzyl     trans-3-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]cyclobutanecarboxylate; -   N-[4-(4-{[(4-methylpiperazin-1-yl)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(benzoylamino)cyclohex-1-en-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1-methylpiperidin-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3R)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3S)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-2-methylbutanoyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(3-methylbutanoyl)amino]oxetan-3-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   tert-butyl     4-({4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}sulfonyl)piperidine-1-carboxylate; -   N-{4-[4-(propylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methoxyethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclopentylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(1,4-dioxan-2-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopentylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(morpholin-4-ylcarbonyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopropylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(butan-2-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{(4R)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(4S)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[trans-3-(benzylcarbamoyl)cyclobutyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{trans-3-[(2-phenylethyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{trans-3-[(3-phenylpropyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methyl-1,3-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(furan-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-3-(furan-2-yl)prop-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,3-oxazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3,3,3-trifluoropropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,5-dimethyl-1H-pyrazol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methoxycyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-difluorocyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1H-pyrazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tert-butoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-1,2,4-triazol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-ethoxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-hydroxy-3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-pyrrol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methylpropoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1-methylprolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-hydroxycyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-{[1-(methoxymethyl)cyclopropyl]carbonyl}-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(methylsulfonyl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-4-methylpent-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-methoxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopent-1-en-1-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(thiophen-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-propanoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4-methylhexanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-dimethylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclobutylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(piperidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[2-(pyrrolidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(bicyclo[2.2.1]hept-2-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopentylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds of Formula (Ic), which are

-   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds of Formula (Ic), which are

-   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIc)

In another aspect, the present invention provides compounds of Formula (IIc)

and pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (Ic); and R² is phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the R² phenyl, heterocyclyl, cycloalkyl, and cycloalkenyl are optionally substituted as described herein for substituents on R² in Formula (Ic).

In one embodiment of formula (IIc),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R² is phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when X¹, X², and X³ are CH and R² is phenyl; R⁵ is not methyl;

with the proviso that when X¹, X², and X³ are CH, and R² is phenyl substituted with OR⁵; R⁵ is not methyl;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (IIc), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IIc), X¹, X², and X³ are CH. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IIc), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IIc), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IIc), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IIc), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IIc), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), R¹ is C(O)NH₂. In another embodiment of Formula (IIc), R¹ is F. In another embodiment of Formula (IIc), R¹ is Cl. In another embodiment of Formula (IIc), R¹ is Br. In another embodiment of Formula (IIc), R¹ is CN. In another embodiment of Formula (IIc), R¹ is NH₂. In another embodiment of Formula (IIc), R¹ is NO₂. In another embodiment of Formula (IIc), R¹ is CF₃. In another embodiment of Formula (IIc), R¹ is C(O)OH. In another embodiment of Formula (IIc), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (IIc), which include

-   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(furo[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(thieno[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dihydro-1,4-benzodioxin-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-fluoro-5-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-acetylphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,3-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(6-aminohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-benzodioxol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dihydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-propoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-2-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methyl-1H-indazol-5-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     5-({4[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}amino)-1H-indazole-3-carboxylate; -   N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(5-chloropyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-fluorobenzoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methoxy-1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-propoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(dimethylamino)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoro-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1,3-benzodioxol-5-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-{4-[(2-phenoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-hydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({1-[(3S)-tetrahydrofuran-3-yl]-1H-pyrazol-4-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,4-dioxa-8-azaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylthio)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(trifluoromethyl)thio]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-fluorophenyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(hydroxymethyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-benzodioxol-5-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-isopropyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiomorpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzylpiperidin-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-acetamido-2-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[3-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-imidazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-(3-cyanophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(2-hydroxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyanomethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclohexylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1H-indol-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(phenylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(diethylamino)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-phenylethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-aminophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     (1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}piperidin-4-yl)carbamate; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(cyclohexylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-chlorobenzyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(diethylcarbamoyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-hydroxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-6-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-fluoropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylmethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3,4,9-tetrahydro-2H-beta-carbolin-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tert-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[4-(trifluoromethyl)phenyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-difluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-benzylpyrrolidin-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-carbamoylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopropylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(methylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dioxolan-2-ylmethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(4-fluorophenyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-phenyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(sec-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(ethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isobutyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(trifluoromethyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,6-dimethylmorpholin-4-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(prop-2-yn-1-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyanoethyl)(cyclopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(isopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-N-isopropyl-beta-alanine; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5,6-dimethoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-chlorophenoxy)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate;     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic     acid; -   5-amino-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(aminomethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(2-hydroxy-2-methylpropanoyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetamido-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(N,N-dimethylglycyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methoxyacetyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methylsulfonyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4,4,4-trifluorobutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpentanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(benzyloxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[N-(2-furoyl)glycyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-thienyl)butanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-oxo-4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(N-benzoylglycyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenoxybutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propionylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(heptanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pent-4-enoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-methylpiperazin-1-yl)propanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate; -   2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic     acid; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyclopentylethyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate; -   N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1E)-5-phenylpent-1-en-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[6-(1-propyl-1H-pyrazol-4-yl)pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[1-(3-methylbutyl)-1H-pyrazol-4-yl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-phenylpentyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[2-fluoro-4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{2-fluoro-4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(isopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(isopropylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(benzoylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(butyrylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperazine-1-carboxylate; -   N-[4-(4-propionylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopropylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-butyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-isobutyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(2-benzoyl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[2-(3-methylbutyl)-2,3-dihydro-1H-isoindol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexyloxy)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(5-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-phenylpropyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-phenylpropyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(8-fluoro-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(morpholin-4-ylmethyl)-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-4,5-dihydro-3H-2,3-benzodiazepin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(1-methylpiperidin-4-yl)oxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3R)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3S)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(azetidin-1-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperidine-1-carboxylate; -   N-[4-(5-propyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[5-(3-methylbutyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-benzyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-chloropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-oxopyrrolidin-1-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-hydroxycyclopropyl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]-1H-benzimidazol-2-yl}piperazine-1-carboxylate; -   N-[2-(piperazin-1-yl)-1H-benzimidazol-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-vinyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-benzoylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(tetrahydrofuran-3-yl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-(4-{[(3-phenylpropyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-{4-[1-(4-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(tetrahydrofuran-3-ylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2S)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2R)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-phenylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-methoxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-4-yl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-(2-methoxyethyl)-N²-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-(4-cyanophenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(trifluoromethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(tetrahydrofuran-3-ylmethyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(1,2-dihydroxyethyl)-N-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-butyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide;     and -   N-[2-(4-acetylpiperazin-1-yl)-1H-benzimidazol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-D-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propionyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-chlorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-furoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-thienylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrrol-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2,5-dimethyl-1H-pyrrol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,3-thiazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isonicotinoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridazin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrimidin-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(piperidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[6-(benzoylamino)hexyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(benzoylamino)methyl]benzyl}carbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-L-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-D-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(1-acetylpiperidin-4-yl)carbonyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-acetamidobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(methylsulfonyl)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-butyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isobutyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methylbutanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,3,3-trifluoropropanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(methoxyacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopentylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclohexylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[3-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,4-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,5-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(3,4-dimethoxyphenyl)acetyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrrol-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrazol-5-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isonicotinoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridazin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrazin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrimidin-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(N,N-dimethyl-beta-alanyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-acetylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1,3-thiazol-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(morpholin-4-ylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1-(2-phenylethyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-[2-(dimethylamino)ethyl]-N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(morpholin-4-ylcarbonyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{benzyl[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutoxycarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     4-{[(5-cyano-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoate; -   N-(4-{(E)-[(benzyloxy)imino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-aminopyrrolidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-methylbutyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(3-phenylpropyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-[4-({benzyl[3-(morpholin-4-yl)propyl]amino}methyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-methyl-1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-methoxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-hydroxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(aminomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-(methylthio)butan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3S)-1-hydroxy-3-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3R)-1,3-dihydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxyhexan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2R)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-cyclohexyl-3-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({(2R)-1-hydroxy-3-[(4-methylbenzyl)thio]propan-2-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-tert-butylphenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methoxy-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(2-methoxyethoxy)acetyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[(3-methylbutyl)carbamoyl]pyrazin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(1E)-3-[benzyl(methyl)amino]prop-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-phenoxypiperidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-phenoxyazetidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[benzyl(methyl)amino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[2-(2-oxopyrrolidin-1-yl)ethyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1-benzylpiperidin-4-yl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(morpholin-4-yl)benzyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxypropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-3-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{1′-[(2-methoxyethoxy)acetyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(morpholin-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1-methylpyrrolidin-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(azetidin-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(morpholin-4-ylmethyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methylpiperazin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(3-methylbutyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-hydroxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1-methylpyrrolidin-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-aminoethyl)-1H-imidazol-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2,2-dimethyl-1,3-dioxolan-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-methoxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}-2-oxoethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-{benzyl[3-(morpholin-4-yl)propyl]amino}-3-oxopropyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[1′-(morpholin-4-ylacetyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[1′-(morpholin-4-ylacetyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazol-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2-benzyl-1,3-thiazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-thiazol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(4-methylphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-dihydroxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(ethylsulfonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2,3-dihydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1-hydroxy-4-methylpentan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(5-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.3]hept-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.4]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,9-diazaspiro[5.5]undec-3-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{benzyl[3-(morpholin-4-yl)propyl]amino}-4-oxobutyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetyl-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-hydroxyethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butyrylamino)phenyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methoxybenzyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(2-oxa-7-azaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-(acetamidomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{5-[2-(2-chlorobenzyl)-1,3-thiazol-4-yl]-2-thienyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(2-hydroxypropan-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     {4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzyl}carbamate; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(methoxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(tetrahydrofuran-2-ylmethyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methoxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[4-(2-methoxyethyl)piperazin-1-yl]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-pentanoylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butyrylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(1-acetylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{6-[(1-isobutyrylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(3-methylbutanoyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(methoxyacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     (2-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}ethyl)carbamate; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-phenylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxyphenyl)acetyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-benzoylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-ethoxypropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl[(1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}azetidin-3-yl)methyl]carbamate; -   N-(4-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(morpholin-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2-methoxyethoxy)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(2,3-dimethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxycyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[4-(acetylamino)phenyl]sulfonyl}amino)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(propylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-propylphenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(butylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[({[(1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methyl}sulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(benzylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-fluorophenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(thiophen-2-ylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(N,N-dimethylglycyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(4,4-difluoro     cyclohexyl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-(4-{[1-(1,3-thiazol-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-D-phenylalaninamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(5-methyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-carbamoylbenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide;     Nalpha-{4-[(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(4,5,6,7-tetrahydro-1H-indazol-5-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   5-fluoro-N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanocyclopropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   methyl     1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate; -   N-(4-{3-[(3-methylbutyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydrofuran-2-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(benzylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(cyclopentylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(cyclopentylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(2-methoxyethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrrolidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[(dimethylamino)methyl]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-oxazol-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butanoylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-difluoroethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiophen-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pyrimidin-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-acetylpiperidin-4-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1,3-thiazol-5-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-oxo-4,5,6,7-tetrahydro-1-benzofuran-3-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{2-[(3-methylbutanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(4-methylpentanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(ethoxyacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{[(2-methoxyethoxy)acetyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-2-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[2-(benzoylamino)ethyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-3-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-propanoylazetidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(p     ent-4-ynoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethylglycyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethyl-beta-alanyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrrolidin-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(pyrrolidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methylpiperazin-1-yl)acetyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopropylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopentylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(butylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-fluorophenyl)sulfonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propan-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(benzylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4,4-difluoro     cyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-D-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpentanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridazin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrimidin-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   benzyl     trans-3-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]cyclobutanecarboxylate; -   N-[4-(4-{[(4-methylpiperazin-1-yl)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(benzoylamino)cyclohex-1-en-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1-methylpiperidin-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3R)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3S)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-2-methylbutanoyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(3-methylbutanoyl)amino]oxetan-3-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   tert-butyl     4-({4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}sulfonyl)piperidine-1-carboxylate; -   N-{4-[4-(propylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methoxyethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclopentylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(1,4-dioxan-2-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopentylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(morpholin-4-ylcarbonyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopropylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(butan-2-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{(4R)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(4S)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[trans-3-(benzylcarbamoyl)cyclobutyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{trans-3-[(2-phenylethyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{trans-3-[(3-phenylpropyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methyl-1,3-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(furan-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-3-(furan-2-yl)prop-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,3-oxazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3,3,3-trifluoropropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,5-dimethyl-1H-pyrazol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methoxycyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-difluorocyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1H-pyrazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tert-butoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-1,2,4-triazol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-ethoxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-hydroxy-3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-pyrrol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methylpropoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1-methylprolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-hydroxycyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-{[1-(methoxymethyl)cyclopropyl]carbonyl}-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(methylsulfonyl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-4-methylpent-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-methoxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopent-1-en-1-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(thiophen-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-propanoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4-methylhexanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-dimethylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclobutylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(piperidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[2-(pyrrolidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{6-[(bicyclo[2.2.1]hept-2-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopentylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IIIc)

In another aspect, the present invention provides compounds of Formula (IIIc)

and pharmaceutically acceptable salts thereof; wherein X¹, X², X³, are as described herein for Formula (Ic); and R^(X) is as described herein for substituents at the para position in Formula (Ic) when R² is phenyl.

In one embodiment of formula (IIIc),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R^(x) is R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when X¹, X², and X³ are CH; R^(x) is not methyl;

with the proviso that when X¹, X², and X³ are CH; R^(x) is not methoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (IIIc), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IIIc), X¹, X², and X³ are CH. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IIIc), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IIIc), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IIIc), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IIIc), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IIIc), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IIIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), R¹ is C(O)NH₂. In another embodiment of Formula (IIIc), R¹ is F. In another embodiment of Formula (IIIc), R¹ is Cl. In another embodiment of Formula (IIIc), R¹ is Br. In another embodiment of Formula (IIIc), R¹ is CN. In another embodiment of Formula (IIIc), R¹ is NH₂. In another embodiment of Formula (IIIc), R¹ is NO₂. In another embodiment of Formula (IIIc), R¹ is CF₃. In another embodiment of Formula (IIIc), R¹ is C(O)OH. In another embodiment of Formula (IIIc), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In one embodiment of formula (IIIc), R^(x) is R⁵, OR⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, NHR⁵, NHC(O)R⁵, NHS(O)₂R⁵, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOR⁵, SO₂NHR⁵ or CF₃. In another embodiment of formula (IIIc), R^(x) is R⁵, and R⁵ is heterocyclyl, which is optionally substituted as described in embodiments herein.

In another embodiment of Formula (IIIc), R^(x) is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one, isoindolin-1-onyl, or 1,2,3,6-tetrahydropyridinyl. In another embodiment of Formula (IIIc), R^(x) is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, isoindolin-1-onyl, or pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one; which are optionally substituted as defined herein. In another embodiment of Formula (IIIc), R^(x) is, 2,3,6-tetrahydropyridinyl; which is optionally substituted as defined herein.

Still another embodiment pertains to compounds having Formula (IIIc), which include

-   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(furo[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(thieno[3,2-c]pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dihydro-1,4-benzodioxin-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-fluoro-5-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrimidin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-methoxyphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(4-acetylphenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,3-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(6-aminohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-benzodioxol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridazin-3-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(3-fluorophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dihydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-propoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-cyanophenyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-2-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methyl-1H-indazol-5-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     5-({4[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}amino)-1H-indazole-3-carboxylate; -   N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(5-chloropyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-fluorobenzoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methoxy-1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-propoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(pyridin-4-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(dimethylamino)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoro-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1,3-benzodioxol-5-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-{4-[(2-phenoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-hydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({1-[(3S)-tetrahydrofuran-3-yl]-1H-pyrazol-4-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,4-dioxa-8-azaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylthio)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(trifluoromethyl)thio]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-fluorophenyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(hydroxymethyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-benzodioxol-5-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-isopropyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiomorpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzylpiperidin-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-acetamido-2-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[3-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-imidazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-(3-cyanophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(2-hydroxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyanomethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclohexylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1H-indol-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(phenylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(diethylamino)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-phenylethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-aminophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     (1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}piperidin-4-yl)carbamate; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[3-chloro-5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(cyclohexylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-chlorobenzyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(diethylcarbamoyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-hydroxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-6-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-fluoropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylmethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3,4,9-tetrahydro-2H-beta-carbolin-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tert-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[4-(trifluoromethyl)phenyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-difluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-benzylpyrrolidin-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-carbamoylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopropylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(methylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dioxolan-2-ylmethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(4-fluorophenyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-phenyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(sec-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[butyl(ethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isobutyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-carbamoylphenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(trifluoromethyl)pyrrolidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,6-dimethylmorpholin-4-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethylpyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(prop-2-yn-1-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[isopropyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyanoethyl)(cyclopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[ethyl(isopropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoropyrrolidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-N-isopropyl-beta-alanine; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide;     5,6-dimethoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-chlorophenoxy)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate;     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic     acid; -   5-amino-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(aminomethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(2-hydroxy-2-methylpropanoyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetamido-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(N,N-dimethylglycyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methoxyacetyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methylsulfonyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4,4,4-trifluorobutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpentanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(benzyloxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[N-(2-furoyl)glycyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-thienyl)butanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-oxo-4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(N-benzoylglycyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenoxybutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propionylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(heptanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pent-4-enoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-methylpiperazin-1-yl)propanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate; -   2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic     acid; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-cyclopentylethyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate; -   N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1E)-5-phenylpent-1-en-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-phenylpentyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(isopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(isopropylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(benzoylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[3-(butyrylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperazine-1-carboxylate; -   N-[4-(4-propionylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopropylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexyloxy)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(8-fluoro-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(morpholin-4-ylmethyl)-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-4,5-dihydro-3H-2,3-benzodiazepin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(1-methylpiperidin-4-yl)oxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3R)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3S)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(azetidin-1-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperidine-1-carboxylate; -   N-[4-(5-propyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[5-(3-methylbutyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-benzyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-chloropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-oxopyrrolidin-1-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-hydroxycyclopropyl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-vinyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-benzoylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(tetrahydrofuran-3-yl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-(4-{[(3-phenylpropyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-{4-[1-(4-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(tetrahydrofuran-3-ylmethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2S)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2R)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-phenylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-methoxyethyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-(2-hydroxyethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-4-yl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-(2-methoxyethyl)-N²-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-(4-cyanophenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(trifluoromethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(tetrahydrofuran-3-ylmethyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(1,2-dihydroxyethyl)-N-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-D-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propionyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-chlorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-furoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-thienylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrrol-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2,5-dimethyl-1H-pyrrol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,3-thiazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isonicotinoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridazin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrimidin-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(piperidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[6-(benzoylamino)hexyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(benzoylamino)methyl]benzyl}carbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-L-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(5-oxo-D-prolyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(1-acetylpiperidin-4-yl)carbonyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-acetamidobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(methylsulfonyl)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-butyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isobutyrylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methylbutanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,3,3-trifluoropropanoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(methoxyacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(tetrahydrofuran-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclopentylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(cyclohexylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-methoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-chlorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-cyanobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[3-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[4-(dimethylamino)benzoyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,4-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3,5-dimethoxybenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(3,4-dimethoxyphenyl)acetyl]piperazin-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(3-furoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrrol-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1H-pyrazol-5-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-isonicotinoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyridazin-3-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrazin-2-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(pyrimidin-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(N,N-dimethyl-beta-alanyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-acetylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(2-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(4-fluorobenzoyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(phenylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(1,3-thiazol-4-ylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-(morpholin-4-ylacetyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N⁵-[2-(dimethylamino)ethyl]-N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(morpholin-4-ylcarbonyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{benzyl[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutoxycarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     4-{[(5-cyano-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoate; -   N-(4-{(E)-[(benzyloxy)imino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-aminopyrrolidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-[4-({benzyl[3-(morpholin-4-yl)propyl]amino}methyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-methyl-1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-methoxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-hydroxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(aminomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-(methylthio)butan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3S)-1-hydroxy-3-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3R)-1,3-dihydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxyhexan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2R)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-cyclohexyl-3-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({(2R)-1-hydroxy-3-[(4-methylbenzyl)thio]propan-2-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-tert-butylphenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methoxy-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide;     N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(1E)-3-[benzyl(methyl)amino]prop-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-phenoxypiperidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-phenoxyazetidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[benzyl(methyl)amino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbutyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[2-(2-oxopyrrolidin-1-yl)ethyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1-benzylpiperidin-4-yl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-phenylpropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(morpholin-4-yl)benzyl]-1H-1,2,3-triazol-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylmethyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxypropyl)-1H-1,2,3-triazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-3-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(morpholin-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(azetidin-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[5-(morpholin-4-ylmethyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methylpiperazin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(3-methylbutyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-hydroxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(2-aminoethyl)-1H-imidazol-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2,2-dimethyl-1,3-dioxolan-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-methoxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}-2-oxoethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3-{benzyl[3-(morpholin-4-yl)propyl]amino}-3-oxopropyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2-benzyl-1,3-thiazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-thiazol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(4-methylphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-dihydroxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(2-furoyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(tetrahydrofuran-2-ylcarbonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[4-(ethylsulfonyl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2,3-dihydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1-hydroxy-4-methylpentan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.3]hept-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.4]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(3,9-diazaspiro[5.5]undec-3-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{benzyl[3-(morpholin-4-yl)propyl]amino}-4-oxobutyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetyl-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-hydroxyethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butyrylamino)phenyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methoxybenzyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-6-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.4]oct-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(2-oxa-7-azaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-(acetamidomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(2-hydroxypropan-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     {4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzyl}carbamate; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(methoxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[(tetrahydrofuran-2-ylmethyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{5-[(4-methoxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(5-{[4-(2-methoxyethyl)piperazin-1-yl]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-pentanoylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4[(1-acetylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butyrylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   tert-butyl     (2-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}ethyl)carbamate; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-phenylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxyphenyl)acetyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-benzoylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-ethoxypropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl[(1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}azetidin-3-yl)methyl]carbamate; -   N-(4-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(morpholin-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2-methoxyethoxy)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(2,3-dimethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methoxycyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[4-(acetylamino)phenyl]sulfonyl}amino)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(propylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-propylphenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(butylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[({[(1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methyl}sulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(benzylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-fluorophenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(thiophen-2-ylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(N,N-dimethylglycyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(4,4-difluorocyclohexyl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-(4-{[1-(1,3-thiazol-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-D-phenylalaninamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(5-methyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-carbamoylbenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   Nalpha-{4-[(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(4,5,6,7-tetrahydro-1H-indazol-5-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   5-fluoro-N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[benzyl(methyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4[(2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanocyclopropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[methyl(propyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   methyl     1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate; -   N-(4-{3-[(3-methylbutyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydrofuran-2-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(benzylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[3-(cyclopentylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(cyclopentylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(2-methoxyethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrrolidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[(dimethylamino)methyl]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-oxazol-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-acetylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-butanoylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(methoxyacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclobutylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-difluoroethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;     Nalpha-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[2(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiophen-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pyrimidin-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-acetylpiperidin-4-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1,3-thiazol-5-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-oxo-4,5,6,7-tetrahydro-1-benzofuran-3-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{2-[(3-methylbutanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(4-methylpentanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(ethoxyacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2-{[(2-methoxyethoxy)acetyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-2-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(cyclopentylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[2-(benzoylamino)ethyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydro-2H-pyran-4-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{2-[(tetrahydrofuran-3-ylacetyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-L-prolyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-propanoylazetidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(p     ent-4-ynoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(furan-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethylglycyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(N,N-dimethyl-beta-alanyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrrolidin-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(pyrrolidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-methylpiperazin-1-yl)acetyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopropylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-cyclopentylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3,3-dimethylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclohexylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopentylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(tetrahydrofuran-2-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpropyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(butylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(cyclopropylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(phenylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4-fluorophenyl)sulfonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(ethylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propan-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(benzylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(propylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(4,4-difluorocyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(5-oxo-D-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-methylpentanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(2-ethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyridazin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(pyrimidin-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(piperidin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(4-methylpiperazin-1-yl)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(benzoylamino)cyclohex-1-en-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1-methylpiperidin-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3R)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(3S)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-{[(2S)-2-methylbutanoyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{3-[(3-methylbutanoyl)amino]oxetan-3-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   tert-butyl     4-({4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}sulfonyl)piperidine-1-carboxylate; -   N-{4-[4-(propylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methoxyethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(cyclopentylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(1,4-dioxan-2-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopentylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(morpholin-4-ylcarbonyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(cyclopropylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[4-(butan-2-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{(4R)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{(4S)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methyl-1,3-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(furan-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-3-(furan-2-yl)prop-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,3-oxazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3,3,3-trifluoropropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,5-dimethyl-1H-pyrazol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methoxycyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-difluorocyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1H-pyrazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tert-butoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-1,2,4-triazol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-ethoxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-hydroxy-3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-pyrrol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methylpropoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1-methylprolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-hydroxycyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-{[1-(methoxymethyl)cyclopropyl]carbonyl}-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(methylsulfonyl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-4-methylpent-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-methoxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopent-1-en-1-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(thiophen-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-propanoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4-methylhexanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-dimethylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclobutylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(piperidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[2-(pyrrolidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cis-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(trans-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{trans-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{cis-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopentylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Still another embodiment pertains to compounds having Formula (IIIc), which include

-   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(8-fluoro-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(morpholin-4-ylmethyl)-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-4,5-dihydro-3H-2,3-benzodiazepin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(dimethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(di     ethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(1-methylpiperidin-4-yl)oxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3R)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-{[(3S)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(azetidin-1-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide;     and -   N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IVc)

In another aspect, the present invention provides compounds of Formula (IVc)

and pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (Ic).

In one embodiment of formula (IVc),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, Se, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (IVc), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (IVc), X¹, X², and X³ are CH. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (IVc), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (IVc), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (IVc), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (IVc), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (IVc), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (IVc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), R¹ is C(O)NH₂. In another embodiment of Formula (IVc), R¹ is F. In another embodiment of Formula (IVc), R¹ is Cl. In another embodiment of Formula (IVc), R¹ is Br. In another embodiment of Formula (IVc), R¹ is CN. In another embodiment of Formula (IVc), R¹ is NH₂. In another embodiment of Formula (IVc), R¹ is NO₂. In another embodiment of Formula (IVc), R¹ is CF₃. In another embodiment of Formula (IVc), R¹ is C(O)OH. In another embodiment of Formula (IVc), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (IVc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (IVc), which include

-   N-{4-[(4,4,4-trifluorobutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpentanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(benzyloxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[N-(2-furoyl)glycyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-thienyl)butanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-oxo-4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(N-benzoylglycyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenoxybutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propionylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(hexanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(heptanoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pent-4-enoylamino)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopropylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-methylpiperazin-1-yl)propanoyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate; -   2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic     acid; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-methyl-1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-methoxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-hydroxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(aminomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methoxy-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-3-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-(4-{[(2-methoxyethoxy)acetyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydrofuran-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-{4-[(morpholin-4-ylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-chloro-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetyl-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-hydroxyethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butyrylamino)phenyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   -4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-(acetamidomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(2-hydroxypropan-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(methoxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-acetylpiperidin-4-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1,3-thiazol-5-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(4-oxo-4,5,6,7-tetrahydro-1-benzofuran-3-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Embodiments of Formula (Vc)

In another aspect, the present invention provides compounds of Formula (Vc)

and pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R⁵ are as described herein for Formula (Ic).

In one embodiment of formula (Vc),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (Vc), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (Vc), X¹, X², and X³ are CH. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (Vc), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (Vc), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (Vc), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (Vc), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (Vc), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (Vc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), R¹ is C(O)NH₂. In another embodiment of Formula (Vc), R¹ is F. In another embodiment of Formula (Vc), R¹ is Cl. In another embodiment of Formula (Vc), R¹ is Br. In another embodiment of Formula (Vc), R¹ is CN. In another embodiment of Formula (Vc), R¹ is NH₂. In another embodiment of Formula (Vc), R¹ is NO₂. In another embodiment of Formula (Vc), R¹ is CF₃. In another embodiment of Formula (Vc), R¹ is C(O)OH. In another embodiment of Formula (Vc), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Vc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Vc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (Vc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (Vc), which include

-   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dihydro-1,4-benzodioxin-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5-methyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-fluoro-5-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,3-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-methylbutyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(6-aminohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide;     4-chloro-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-thienyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1,3-benzodioxol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(benzylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dihydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-propoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-2-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methyl-1H-indazol-5-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4[(1-benzyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     5-({4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}amino)-1H-indazole-3-carboxylate; -   N-(4-{[2-(2-oxopyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(2,3-dihydro-1,4-benzodioxin-6-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methoxy-1H-indol-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-propoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4,5-trimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methylpiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(dimethylamino)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(trifluoromethoxy)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluoro-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,3-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1,3-benzodioxol-5-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   4-chloro-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-{4-[(2-phenoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-hydroxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-fluorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({1-[(3S)-tetrahydrofuran-3-yl]-1H-pyrazol-4-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylthio)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(trifluoromethyl)thio]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,4-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-5-(trifluoromethyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(hydroxymethyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-benzodioxol-5-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-isopropyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-ethyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,5-dimethoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-benzylpiperidin-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-acetamido-2-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[3-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-imidazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-(3-cyanophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-cyanophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-chlorophenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(cyanomethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide;     N-[4-(cyclohexylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(phenylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(diethylamino)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-aminophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3-chlorobenzyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-6-methylphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-fluoropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tert-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methylbutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-benzylpyrrolidin-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-fluorophenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopropylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(methylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pentan-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclobutylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(4-fluorophenyl)-1H-pyrazol-4-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-phenyl-1H-pyrazol-4-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[4-(trifluoromethyl)phenyl]ethyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(sec-butylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(prop-2-yn-1-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5,6-dimethoxy-N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(4-chlorophenoxy)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(trifluoromethoxy)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4-phenyl-1,3-thiazol-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   methyl     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate;     2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic     acid; -   5-amino-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(hydroxymethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(aminomethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(2-hydroxy-2-methylpropanoyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-acetamido-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(N,N-dimethylglycyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methoxyacetyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-[(methylsulfonyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-bromo-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(5-chloropyridin-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-hydroxy-4-methoxyphenyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,4-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(2-oxopyrrolidin-1-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-hydroxycyclopropyl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-5-vinyl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   N-(4-{[(3-phenylpropyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-d]pyrimidine-6-carboxamide; -   5-fluoro-N-[4-({[(2S)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-({[(2R)-tetrahydrofuran-2-ylmethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-phenylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-4-yl-1,3-dihydro-2H-isoindole-2-carboxamide; -   N⁵-(2-methoxyethyl)-N²-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(tetrahydrofuran-3-ylmethyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-({[(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-(1,2-dihydroxyethyl)-N-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[6-(benzoylamino)hexyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({4-[(benzoylamino)methyl]benzyl}carbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N⁵-[2-(dimethylamino)ethyl]-N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide; -   5-(morpholin-4-ylcarbonyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(isobutoxycarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-(methylthio)butan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3S)-1-hydroxy-3-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S,3R)-1,3-dihydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxyhexan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-hydroxypentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2S)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S,2R)-2-hydroxycyclopentyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-cyclohexyl-3-hydroxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({(2R)-1-hydroxy-3-[(4-methylbenzyl)thio]propan-2-yl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(4-tert-butylphenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methoxy-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-methyl-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   5-(hydroxymethyl)-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   5-fluoro-N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2,2-dimethyl-1,3-dioxolan-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-methoxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-thiazol-5-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-3-hydroxy-1-phenylpropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(4-methylphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1,3-dihydroxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(3-furylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1R)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(2S)-1-hydroxybutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(2,3-dihydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(1-hydroxy-4-methylpentan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-{4[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-fluoro-N-(4-{[1-(1,3-thiazol-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-D-phenylalaninamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   Nalpha-(4-{[(5-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoyl)-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(5-methyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-carbamoylbenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   Nalpha-{4-[(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(4,5,6,7-tetrahydro-1H-indazol-5-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   5-fluoro-N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2R)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-1-amino-1-oxobutan-2-yl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-fluoro-N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanocyclopropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; -   N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(4,4-difluorocyclohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(ethylamino)-1-oxopropan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,3-oxazol-2-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-({2-[(dimethylamino)methyl]benzyl}carbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1R)-2-amino-2-oxo-1-phenylethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1,3-oxazol-2-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(furan-2-yl)-2-(pyrrolidin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(3,5-dimethyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2,2-difluoroethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(5-methyl-1,2-oxazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide;     Nalpha-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; -   N-(4-{[2-(2-methyl-1,3-thiazol-4-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3,3-dimethyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(thiophen-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(3-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(acetylamino)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(pyrimidin-4-ylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-2-methylbutyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-amino-2-oxo-1-phenylethyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[3-(methylcarbamoyl)phenyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[(2S)-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-1-(morpholin-4-yl)propan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIc)

In another aspect, the present invention provides compounds of Formula (VIc)

and pharmaceutically acceptable salts thereof; wherein R¹ and R⁵ are as described herein for Formula (Ic); and n is 0 or 1.

In one embodiment of formula (VIc),

n is 0 or 1;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁹, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.

In another embodiment of Formula (VIc), n is 0. In another embodiment of Formula (VIc), n is 1. In another embodiment of Formula (VIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIc), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIc), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIc), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIc), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIc), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIc), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIc), R¹ is C(O)NH₂. In another embodiment of Formula (VIc), R¹ is F. In another embodiment of Formula (VIc), R¹ is Cl. In another embodiment of Formula (VIc), R¹ is Br. In another embodiment of Formula (VIc), R¹ is CN. In another embodiment of Formula (VIc), R¹ is NH₂. In another embodiment of Formula (VIc), R¹ is NO₂. In another embodiment of Formula (VIc), R¹ is CF₃. In another embodiment of Formula (VIc), R¹ is C(O)OH. In another embodiment of Formula (VIc), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (VIc), which include

-   N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-([(1S)-2-hydroxy-1-phenylethyl]amino     carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-([(1S)-2-hydroxy-1-pyridin-2-ylethyl]amino     carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(azetidin-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIIc)

In another aspect, the present invention provides compounds of Formula (VIIc)

and pharmaceutically acceptable salts thereof; wherein X¹, X², X³, and R¹³ are as described herein for Formula (Ic), and

indicates a single or a double bond.

In one embodiment of formula (VIIc),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

indicates a single or double bond;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

wherein the cyclic moieties represented by R³, R⁶, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (VIIc), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (VIIc), X¹, X², and X³ are CH. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (VIIc), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (VIIc), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (VIIc), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (VIIc), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (VIIc), X¹ is N; X² is CR¹; and X³ is N.

In one embodiment of Formula (VIIc),

is a single bond. In another embodiment of Formula (VIIc),

is a double bond.

In another embodiment of Formula (VIIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), R¹ is C(O)NH₂. In another embodiment of Formula (VIIc), R¹ is F. In another embodiment of Formula (VIIc), R¹ is Cl. In another embodiment of Formula (VIIc), R¹ is Br. In another embodiment of Formula (VIIc), R¹ is CN. In another embodiment of Formula (VIIc), R¹ is NH₂. In another embodiment of Formula (VIIc), R¹ is NO₂. In another embodiment of Formula (VIIc), R¹ is CF₃. In another embodiment of Formula (VIIc), R¹ is C(O)OH. In another embodiment of Formula (VIIc), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

Still another embodiment pertains to compounds having Formula (VIIc), which include

-   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   tert-butyl     4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperidine-1-carboxylate; -   N-[4-(1-butyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(5-oxo-D-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-propionyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(ethoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-methoxybenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-fluorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(4-chlorobenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[4-(dimethylamino)benzoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(3-thienylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrrol-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2,5-dimethyl-1H-pyrrol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,3-thiazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1H-pyrazol-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-isonicotinoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridazin-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyrimidin-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[3-(piperidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(N,N-dimethylglycyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydro-2H-pyran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrrolidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   5-cyano-N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-(4-{1-[(2-methyl-1,3-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(furan-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-3-(furan-2-yl)prop-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1,3-oxazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3,3,3-trifluoropropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,5-dimethyl-1H-pyrazol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4-methoxycyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-difluorocyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1H-pyrazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tert-butoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-1,2,4-triazol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-ethoxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(3-hydroxy-3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[3-(1H-pyrrol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methylpropoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(1-methylprolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-hydroxycyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-{[1-(methoxymethyl)cyclopropyl]carbonyl}-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(methylsulfonyl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2E)-4-methylpent-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-methoxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopent-1-en-1-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(thiophen-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-[4-(1-propanoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2,2-dimethylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4-methylhexanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2,2-dimethylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclobutylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(piperidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[2-(pyrrolidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,3-dimethyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VIIIc)

One embodiment of this invention, therefore, pertains to compounds or pharmaceutically acceptable salts thereof, which are useful as inhibitors of NAMPT, the compounds having Formula (VIIIc)

wherein

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

X¹ is CH; X² is N; and X³ is CR¹; or

X¹ is CR¹; X² is N; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is CH; or

X¹ is N; X² is CR¹; and X³ is N;

R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂;

R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R⁸, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁸ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R¹²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I;

R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl;

R¹², at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹² alkyl, alkenyl, and alkynyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁶, R⁸, R¹⁰, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I; wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy;

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In one embodiment of Formula (VIIIc), X¹, X², and X³ are CH; or X¹ and X³ are CH; and X² is N; or X¹ and X³ are CH; and X² is CR¹; or X² and X³ are CH; and X¹ is CR¹; or X¹ is CH; and X² and X³ are CR¹; or X² is CH; and X¹ and X³ are N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N. In another embodiment of Formula (VIIIc), X¹, X², and X³ are CH. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is N. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹. In another embodiment of Formula (VIIIc), X² is CH; and X¹ and X³ are N. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is N. In another embodiment of Formula (VIIIc), X¹ is CH; X² is N; and X³ is CR¹. In another embodiment of Formula (VIIIc), X¹ is CR¹; X² is N; and X³ is CH. In another embodiment of Formula (VIIIc), X¹ is N; X² is CR¹; and X³ is CH. In another embodiment of Formula (VIIIc), X¹ is N; X² is CR¹; and X³ is N.

In another embodiment of Formula (VIIIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIIc), R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), R¹ is C(O)NH₂. In another embodiment of Formula (VIIIc), R¹ is F. In another embodiment of Formula (VIIIc), R¹ is Cl. In another embodiment of Formula (VIIIc), R¹ is Br. In another embodiment of Formula (VIIIc), R¹ is CN. In another embodiment of Formula (VIIIc), R¹ is NH₂. In another embodiment of Formula (VIIIc), R¹ is NO₂. In another embodiment of Formula (VIIIc), R¹ is CF₃. In another embodiment of Formula (VIIIc), R¹ is C(O)OH. In another embodiment of Formula (VIIIc), R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is F. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Cl. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is Br. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CN. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIIc), X¹ and X³ are CH; and X² is CR¹; R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is F. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Cl. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is Br. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CN. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIIc), X² and X³ are CH; and X¹ is CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is R³, OR³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)OR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is C(O)NHR³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHC(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; R¹ is NHSO₂R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; wherein R⁶ is alkyl or heterocyclyl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)NH₂. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is F. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Cl. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is Br. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CN. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NH₂. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is NO₂. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is CF₃. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)OH. In another embodiment of Formula (VIIIc), X¹ is CH; and X² and X³ are CR¹; and R¹ is C(O)R³; wherein R³ is alkyl, alkenyl, or heterocyclyl; wherein each alkyl is optionally substituted with one or more independently selected R⁶, OR⁶, NH₂, NHC(O)R⁶, N(R⁶)₂, or OH; and R⁶ is alkyl or heterocyclyl.

In one embodiment of Formula (VIIIc),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R³, at each occurrence, is independently selected alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, OH, F, Cl, Br or I;

R⁶, at each occurrence, is independently selected alkyl or heterocyclyl; wherein each R⁶ alkyl is optionally substituted with one, two, three or four independently selected F, Cl, Br or I;

R⁸, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁸ alkyl is optionally substituted with one, two, three or four independently selected R¹², OR¹²OH, CF₃, F, Cl, Br or I;

R¹², at each occurrence, is independently selected alkyl, heterocyclyl, or cycloalkyl; wherein each R¹² alkyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁶, R⁸, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, Cl, Br or I;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SO₂R¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NHC(O)OR¹⁴, OH, CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, OH, CN, CF₃, F, Cl, Br or I;

R¹⁴, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, OH, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

In another embodiment of Formula (VIIIc),

X¹, X², and X³ are CH; or

X¹ and X³ are CH; and X² is N; or

X¹ and X³ are CH; and X² is CR¹; or

X² and X³ are CH; and X¹ is CR¹; or

X¹ is CH; and X² and X³ are CR¹; or

X² is CH; and X¹ and X³ are N; or

X² and X³ are CH; and X¹ is N; or

R¹ is R³, OR³, C(O)R³, C(O)OR³, C(O)NH₂, C(O)NHR³, NHC(O)R³, NHSO₂R³, F, Cl, Br, I, CN, NH₂, NO₂, CF₃, or C(O)OH;

R³, at each occurrence, is independently selected alkyl, alkenyl, or heterocyclyl; wherein each R³ alkyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, NH₂, N(R⁶)₂, NHC(O)R⁶, or OH;

R⁶, at each occurrence, is independently selected alkyl or heterocyclyl; R⁸, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R⁸ alkyl is optionally substituted with one, two, three or four independently selected R¹², OR¹²OH, or CF₃;

R¹², at each occurrence, is independently selected alkyl, heterocyclyl, or cycloalkyl; wherein each R¹² alkyl is optionally substituted with one or more alkoxy;

wherein the cyclic moieties represented by R³, R⁶, R⁸, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, NH₂, N(R¹³)₂, NHC(O)R¹³, NHC(O)OR¹³, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, OH, CN, CF₃, OCF₃, SCF₃, F, or Cl;

R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SO₂R¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂), NHC(O)R¹⁴, NHC(O)OR¹⁴, OH, or CF₃; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SO₂R¹⁵, C(O)R¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, CN, OH, CF₃, F, or Cl;

R¹⁴, at each occurrence, is independently selected alkyl, aryl, heterocyclyl, or cycloalkyl; wherein each R¹⁴ alkyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, or OH; wherein each R¹⁴ aryl, heterocyclyl, and cycloalkyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, or Cl;

R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and

R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four independently selected alkoxy;

with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl; and

with the proviso that when R¹³ is pyrrolinyl, at least one of X¹, X², and X³ is N.

Still another embodiment pertains to compounds having Formula (VIIIc), which include

-   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-{4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide; -   N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-chlorobenzoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclohexylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(cyclopropylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; -   N-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide;     and pharmaceutically acceptable salts thereof.     Pharmaceutical Compositions, Combination Therapies, Methods of     Treatment, and Administration

Another embodiment comprises pharmaceutical compositions comprising a compound having Formula (I) and an excipient.

Still another embodiment comprises methods of treating cancer in a mammal comprising administering thereto a therapeutically acceptable amount of a compound having Formula (I).

Still another embodiment pertains to compositions for treating diseases during which NAMPT is expressed, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I).

Still another embodiment pertains to compositions for treating diseases during which ROCK is expressed, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I).

Still another embodiment pertains to methods of treating disease in a patient during which NAMPT is expressed, said methods comprising administering to the patient a therapeutically effective amount of a compound having Formula (I).

Still another embodiment pertains to methods of treating disease in a patient during which ROCK is expressed, said methods comprising administering to the patient a therapeutically effective amount of a compound having Formula (I).

Still another embodiment pertains to compositions for treating inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I).

Still another embodiment pertains to compositions for treating hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, spinal-cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, Alzheimer's disease, pain, multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, preterm labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive compulsive disorder and bipolar disorder, epilepsy and seizure disorders, for decreasing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for the prevention of graft failure, and cystic fibrosis, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I).

Still another embodiment pertains to methods of treating inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia in a patient, said methods comprising administering to the patient a therapeutically effective amount of a compound having Formula (I).

Still another embodiment pertains to methods of treating hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, spinal-cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, Alzheimer's disease, pain, multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, preterm labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive compulsive disorder and bipolar disorder, epilepsy and seizure disorders, for decreasing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for the prevention of graft failure, and cystic fibrosis, said methods comprising administering to the patient a therapeutically effective amount of a compound having Formula (I).

Still another embodiment pertains to compositions for treating diseases during which NAMPT is expressed, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to compositions for treating diseases during which ROCK is expressed, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating disease in a patient during which NAMPT is expressed, said methods comprising administering to the patient a therapeutically effective amount of a compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating disease in a patient during which ROCK is expressed, said methods comprising administering to the patient a therapeutically effective amount of a compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to compositions for treating inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to compositions for treating hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, spinal-cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, Alzheimer's disease, pain, multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, preterm labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive compulsive disorder and bipolar disorder, epilepsy and seizure disorders, for decreasing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for the prevention of graft failure, and cystic fibrosis, said compositions comprising an excipient and a therapeutically effective amount of the compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia in a patient, said methods comprising administering to the patient a therapeutically effective amount of the compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating hypertension, chronic and congestive heart failure, cardiac hypertrophy, restenosis, chronic renal failure, cerebral vasospasm after subarachnoid bleeding, pulmonary hypertension, atherosclerosis, asthma, male erectile dysfunctions, female sexual dysfunction, over-active bladder syndrome, spinal-cord injury, traumatic brain injury, stroke, inflammatory and demyelinating diseases, Alzheimer's disease, pain, multiple sclerosis, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease, inflammatory pain, rheumatoid arthritis, osteoarthritis, irritable bowel syndrome, Crohn's disease, psoriasis, ulcerative colitis, lupus, inflammatory bowel disease, cancer, tumor metastasis, viral infections, bacterial infections, insulin resistance, diabetes, ocular hypertension, preterm labor, atherosclerosis, spinal muscular atrophy, encephalomyelitis, osteoporosis, HIV-1, encephalitis, ischemic CNS disorders, vascular or AD type dementia, glaucoma, retinopathy, benign prostatic hypertrophy, psychiatric disorders, in particular depression, schizophrenia, obsessive compulsive disorder and bipolar disorder, epilepsy and seizure disorders, for decreasing ischemia-reperfusion injury, myocardial infarct size and myocardial fibrosis, for the prevention of graft failure, and cystic fibrosis in a patient, said methods comprising administering to the patient a therapeutically effective amount of the compound having Formula (I) and a therapeutically effective amount of one additional therapeutic agent or more than one additional therapeutic agent.

Metabolites of compounds having Formula (I), produced by in vitro or in vivo metabolic processes, may also have utility for treating diseases associated with NAMPT.

Metabolites of compounds having Formula (I), produced by in vitro or in vivo metabolic processes, may also have utility for treating diseases associated with ROCK.

Certain precursor compounds which may be metabolized in vitro or in vivo to form compounds having Formula (I) may also have utility for treating diseases associated with NAMPT.

Certain precursor compounds which may be metabolized in vitro or in vivo to form compounds having Formula (I) may also have utility for treating diseases associated with ROCK.

Compounds having Formula (I) may exist as acid addition salts, basic addition salts or zwitterions. Salts of the compounds are prepared during isolation or following purification of the compounds. Acid addition salts of the compounds are those derived from the reaction of the compounds with an acid. For example, the acetate, adipate, alginate, bicarbonate, citrate, aspartate, benzoate, benzenesulfonate, bisulfate, butyrate, camphorate, camphorsufonate, digluconate, formate, fumarate, glycerophosphate, glutamate, hemisulfate, heptanoate, hexanoate, hydrochloride, hydrobromide, hydroiodide, lactobionate, lactate, maleate, mesitylenesulfonate, methanesulfonate, naphthylenesulfonate, nicotinate, oxalate, pamoate, pectinate, persulfate, phosphate, picrate, propionate, succinate, tartrate, thiocyanate, trichloroacetic, trifluoroacetic, para-toluenesulfonate, and undecanoate salts of the compounds are contemplated as being embraced by this invention. Basic addition salts of the compounds are those derived from the reaction of the compounds with the hydroxide, carbonate or bicarbonate of cations such as lithium, sodium, potassium, calcium, and magnesium.

The compounds having Formula (I) may be administered, for example, bucally, ophthalmically, orally, osmotically, parenterally (intramuscularly, intraperitoneally intrasternally, intravenously, subcutaneously), rectally, topically, transdermally or vaginally.

Therapeutically effective amounts of compounds having Formula (I) depend on the recipient of the treatment, the disorder being treated and the severity thereof, the composition containing the compound, the time of administration, the route of administration, the duration of treatment, the compound potency, its rate of clearance and whether or not another drug is co-administered. The amount of a compound of this invention having Formula (I) used to make a composition to be administered daily to a patient in a single dose or in divided doses is from about 0.03 to about 200 mg/kg body weight. Single dose compositions contain these amounts or a combination of submultiples thereof.

Compounds having Formula (I) may be administered with or without an excipient. Excipients include, for example, encapsulating materials or additives such as absorption accelerators, antioxidants, binders, buffers, coating agents, coloring agents, diluents, disintegrating agents, emulsifiers, extenders, fillers, flavoring agents, humectants, lubricants, perfumes, preservatives, propellants, releasing agents, sterilizing agents, sweeteners, solubilizers, wetting agents and mixtures thereof.

Excipients for preparation of compositions comprising a compound having Formula (I) to be administered orally in solid dosage form include, for example, agar, alginic acid, aluminum hydroxide, benzyl alcohol, benzyl benzoate, 1,3-butylene glycol, carbomers, castor oil, cellulose, cellulose acetate, cocoa butter, corn starch, corn oil, cottonseed oil, cross-povidone, diglycerides, ethanol, ethyl cellulose, ethyl laureate, ethyl oleate, fatty acid esters, gelatin, germ oil, glucose, glycerol, groundnut oil, hydroxypropylmethyl cellulose, isopropanol, isotonic saline, lactose, magnesium hydroxide, magnesium stearate, malt, mannitol, monoglycerides, olive oil, peanut oil, potassium phosphate salts, potato starch, povidone, propylene glycol, Ringer's solution, safflower oil, sesame oil, sodium carboxymethyl cellulose, sodium phosphate salts, sodium lauryl sulfate, sodium sorbitol, soybean oil, stearic acids, stearyl fumarate, sucrose, surfactants, talc, tragacanth, tetrahydrofurfuryl alcohol, triglycerides, water, and mixtures thereof. Excipients for preparation of compositions comprising a compound of this invention having Formula (I) to be administered ophthalmically or orally in liquid dosage forms include, for example, 1,3-butylene glycol, castor oil, corn oil, cottonseed oil, ethanol, fatty acid esters of sorbitan, germ oil, groundnut oil, glycerol, isopropanol, olive oil, polyethylene glycols, propylene glycol, sesame oil, water and mixtures thereof. Excipients for preparation of compositions comprising a compound of this invention having Formula (I) to be administered osmotically include, for example, chlorofluorohydrocarbons, ethanol, water and mixtures thereof. Excipients for preparation of compositions comprising a compound of this invention having Formula (I) to be administered parenterally include, for example, 1,3-butanediol, castor oil, corn oil, cottonseed oil, dextrose, germ oil, groundnut oil, liposomes, oleic acid, olive oil, peanut oil, Ringer's solution, safflower oil, sesame oil, soybean oil, U.S.P. or isotonic sodium chloride solution, water and mixtures thereof. Excipients for preparation of compositions comprising a compound of this invention having Formula (I) to be administered rectally or vaginally include, for example, cocoa butter, polyethylene glycol, wax and mixtures thereof.

Compounds having Formula (I) are expected to be useful when used with alkylating agents, angiogenesis inhibitors, antibodies, antimetabolites, antimitotics, antiproliferatives, antivirals, aurora kinase inhibitors, apoptosis promoters (for example, Bcl-xL, Bcl-w and Bfl-1) inhibitors, activators of death receptor pathway, Bcr-Abl kinase inhibitors, BiTE (Bi-Specific T cell Engager) antibodies, antibody drug conjugates, biologic response modifiers, cyclin-dependent kinase inhibitors, cell cycle inhibitors, cyclooxygenase-2 inhibitors, DVDs, leukemia viral oncogene homolog (ErbB2) receptor inhibitors, growth factor inhibitors, heat shock protein (HSP)-90 inhibitors, histone deacetylase (HDAC) inhibitors, hormonal therapies, immunologicals, inhibitors of inhibitors of apoptosis proteins (IAPs), intercalating antibiotics, kinase inhibitors, kinesin inhibitors, Jak2 inhibitors, mammalian target of rapamycin inhibitors, microRNA's, mitogen-activated extracellular signal-regulated kinase inhibitors, multivalent binding proteins, non-steroidal anti-inflammatory drugs (NSAIDs), poly ADP (adenosine diphosphate)-ribose polymerase (PARP) inhibitors, platinum chemotherapeutics, polo-like kinase (Plk) inhibitors, phosphoinositide-3 kinase (PI3K) inhibitors, proteosome inhibitors, purine analogs, pyrimidine analogs, receptor tyrosine kinase inhibitors, retinoids/deltoids plant alkaloids, small inhibitory ribonucleic acids (siRNAs), topoisomerase inhibitors, ubiquitin ligase inhibitors, and the like, and in combination with one or more of these agents.

BiTE antibodies are bi-specific antibodies that direct T-cells to attack cancer cells by simultaneously binding the two cells. The T-cell then attacks the target cancer cell. Examples of BiTE antibodies include adecatumumab (Micromet MT201), blinatumomab (Micromet MT103) and the like. Without being limited by theory, one of the mechanisms by which T-cells elicit apoptosis of the target cancer cell is by exocytosis of cytolytic granule components, which include perforin and granzyme B. In this regard, Bcl-2 has been shown to attenuate the induction of apoptosis by both perforin and granzyme B. These data suggest that inhibition of Bcl-2 could enhance the cytotoxic effects elicited by T-cells when targeted to cancer cells (V. R. Sutton, D. L. Vaux and J. A. Trapani, J. of Immunology 1997, 158 (12), 5783).

SiRNAs are molecules having endogenous RNA bases or chemically modified nucleotides. The modifications do not abolish cellular activity, but rather impart increased stability and/or increased cellular potency. Examples of chemical modifications include phosphorothioate groups, 2′-deoxynucleotide, 2′-OCH₃-containing ribonucleotides, 2′-F-ribonucleotides, 2′-methoxyethyl ribonucleotides, combinations thereof and the like. The siRNA can have varying lengths (e.g., 10-200 bps) and structures (e.g., hairpins, single/double strands, bulges, nicks/gaps, mismatches) and are processed in cells to provide active gene silencing. A double-stranded siRNA (dsRNA) can have the same number of nucleotides on each strand (blunt ends) or asymmetric ends (overhangs). The overhang of 1-2 nucleotides can be present on the sense and/or the antisense strand, as well as present on the 5′- and/or the 3′-ends of a given strand.

Multivalent binding proteins are binding proteins comprising two or more antigen binding sites. Multivalent binding proteins are engineered to have the three or more antigen binding sites and are generally not naturally occurring antibodies. The term “multispecific binding protein” means a binding protein capable of binding two or more related or unrelated targets. Dual variable domain (DVD) binding proteins are tetravalent or multivalent binding proteins binding proteins comprising two or more antigen binding sites. Such DVDs may be monospecific (i.e., capable of binding one antigen) or multispecific (i.e., capable of binding two or more antigens). DVD binding proteins comprising two heavy chain DVD polypeptides and two light chain DVD polypeptides are referred to as DVD Ig's. Each half of a DVD Ig comprises a heavy chain DVD polypeptide, a light chain DVD polypeptide, and two antigen binding sites. Each binding site comprises a heavy chain variable domain and a light chain variable domain with a total of 6 CDRs involved in antigen binding per antigen binding site.

Alkylating agents include altretamine, AMD-473, AP-5280, apaziquone, bendamustine, brostallicin, busulfan, carboquone, carmustine (BCNU), chlorambucil, CLORETAZINE® (laromustine, VNP 40101M), cyclophosphamide, decarbazine, estramustine, fotemustine, glufosfamide, ifosfamide, KW-2170, lomustine (CCNU), mafosfamide, melphalan, mitobronitol, mitolactol, nimustine, nitrogen mustard N-oxide, ranimustine, temozolomide, thiotepa, TREANDA® (bendamustine), treosulfan, trofosfamide and the like.

Angiogenesis inhibitors include endothelial-specific receptor tyrosine kinase (Tie-2) inhibitors, epidermal growth factor receptor (EGFR) inhibitors, insulin growth factor-2 receptor (IGFR-2) inhibitors, matrix metalloproteinase-2 (MMP-2) inhibitors, matrix metalloproteinase-9 (MMP-9) inhibitors, platelet-derived growth factor receptor (PDGFR) inhibitors, thrombospondin analogs, vascular endothelial growth factor receptor tyrosine kinase (VEGFR) inhibitors and the like.

Antimetabolites include ALIMTA® (pemetrexed disodium, LY231514, MTA), 5-azacitidine, XELODA® (capecitabine), carmofur, LEUSTAT® (cladribine), clofarabine, cytarabine, cytarabine ocfosfate, cytosine arabinoside, decitabine, deferoxamine, doxifluridine, eflornithine, EICAR (5-ethynyl-1-(3-D-ribofuranosylimidazole-4-carboxamide), enocitabine, ethnylcytidine, fludarabine, 5-fluorouracil alone or in combination with leucovorin, GEMZAR® (gemcitabine), hydroxyurea, ALKERAN®(melphalan), mercaptopurine, 6-mercaptopurine riboside, methotrexate, mycophenolic acid, nelarabine, nolatrexed, ocfosfate, pelitrexol, pentostatin, raltitrexed, Ribavirin, triapine, trimetrexate, S-1, tiazofurin, tegafur, TS-1, vidarabine, UFT and the like.

Antivirals include ritonavir, hydroxychloroquine and the like.

Aurora kinase inhibitors include ABT-348, AZD-1152, MLN-8054, VX-680, Aurora A-specific kinase inhibitors, Aurora B-specific kinase inhibitors and pan-Aurora kinase inhibitors and the like.

Bcl-2 protein inhibitors include AT-101 ((−)gossypol), GENASENSE® (G3139 or oblimersen (Bcl-2-targeting antisense oligonucleotide)), IPI-194, IPI-565, N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-nitrobenzenesulfonamide) (ABT-737), N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide (ABT-263), GX-070 (obatoclax) and the like.

Bcr-Abl kinase inhibitors include DASATINIB® (BMS-354825), GLEEVEC® (imatinib) and the like.

CDK inhibitors include AZD-5438, BMI-1040, BMS-032, BMS-387, CVT-2584, flavopyridol, GPC-286199, MCS-5A, PD0332991, PHA-690509, seliciclib (CYC-202, R-roscovitine), ZK-304709 and the like.

COX-2 inhibitors include ABT-963, ARCOXIA® (etoricoxib), BEXTRA® (valdecoxib), BMS347070, CELEBREX® (celecoxib), COX-189 (lumiracoxib), CT-3, DERAMAXX® (deracoxib), JTE-522, 4-methyl-2-(3,4-dimethylphenyl)-1-(4-sulfamoylphenyl-1H-pyrrole), MK-663 (etoricoxib), NS-398, parecoxib, RS-57067, SC-58125, SD-8381, SVT-2016, S-2474, T-614, VIOXX® (rofecoxib) and the like.

EGFR inhibitors include ABX-EGF, anti-EGFR immunoliposomes, EGF-vaccine, EMD-7200, ERBITUX® (cetuximab), HR³, IgA antibodies, IRESSA® (gefitinib), TARCEVA® (erlotinib or OSI-774), TP-38, EGFR fusion protein, TYKERB® (lapatinib) and the like.

ErbB2 receptor inhibitors include CP-724-714, CI-1033 (canertinib), HERCEPTIN® (trastuzumab), TYKERB® (lapatinib), OMNITARG® (2C4, petuzumab), TAK-165, GW-572016 (ionafarnib), GW-282974, EKB-569, PI-166, dHER2 (HER2 vaccine), APC-8024 (HER-2 vaccine), anti-HER/2neu bispecific antibody, B7.her2IgG3, AS HER2 trifunctional bispecfic antibodies, mAB AR-209, mAB 2B-1 and the like.

Histone deacetylase inhibitors include depsipeptide, LAQ-824, MS-275, trapoxin, suberoylanilide hydroxamic acid (SAHA), TSA, valproic acid and the like.

HSP-90 inhibitors include 17-AAG-nab, 17-AAG, CNF-101, CNF-1010, CNF-2024, 17-DMAG, geldanamycin, IPI-504, KOS-953, MYCOGRAB® (human recombinant antibody to HSP-90), NCS-683664, PU24FCl, PU-3, radicicol, SNX-2112, STA-9090 VER49009 and the like.

Inhibitors of inhibitors of apoptosis proteins include HGS1029, GDC-0145, GDC-0152, LCL-161, LBW-242 and the like.

Antibody drug conjugates include anti-CD22-MC-MMAF, anti-CD22-MC-MMAE, anti-CD22-MCC-DM1, CR-011-vcMMAE, PSMA-ADC, MEDI-547, SGN-19Am SGN-35, SGN-75 and the like.

Activators of death receptor pathway include TRAIL, antibodies or other agents that target TRAIL or death receptors (e.g., DR4 and DR5) such as Apomab, conatumumab, ETR2-ST01, GDC0145 (lexatumumab), HGS-1029, LBY-135, PRO-1762 and trastuzumab.

Kinesin inhibitors include Eg5 inhibitors such as AZD4877, ARRY-520; CENPE inhibitors such as GSK923295A and the like.

JAK-2 inhibitors include CEP-701 (lesaurtinib), XL019 and INCB018424 and the like.

MEK inhibitors include ARRY-142886, ARRY-438162 PD-325901, PD-98059 and the like.

mTOR inhibitors include AP-23573, CCI-779, everolimus, RAD-001, rapamycin, temsirolimus, ATP-competitive TORC1/TORC2 inhibitors, including PI-103, PP242, PP30, Torin 1 and the like.

Non-steroidal anti-inflammatory drugs include AMIGESIC® (salsalate), DOLOBID® (diflunisal), MOTRIN® (ibuprofen), ORUDIS® (ketoprofen), RELAFEN® (nabumetone), FELDENE® (piroxicam), ibuprofen cream, ALEVE® (naproxen) and NAPROSYN® (naproxen), VOLTAREN® (diclofenac), INDOCIN® (indomethacin), CLINORIL® (sulindac), TOLECTIN® (tolmetin), LODINE® (etodolac), TORADOL® (ketorolac), DAYPRO® (oxaprozin) and the like.

PDGFR inhibitors include C-451, CP-673, CP-868596 and the like.

Platinum chemotherapeutics include cisplatin, ELOXATIN® (oxaliplatin) eptaplatin, lobaplatin, nedaplatin, PARAPLATIN® (carboplatin), satraplatin, picoplatin and the like.

Polo-like kinase inhibitors include BI-2536 and the like.

Phosphoinositide-3 kinase (PI3K) inhibitors include wortmannin, LY294002, XL-147, CAL-120, ONC-21, AEZS-127, ETP-45658, PX-866, GDC-0941, BGT226, BEZ235, XL765 and the like.

Thrombospondin analogs include ABT-510, ABT-567, ABT-898, TSP-1 and the like.

VEGFR inhibitors include AVASTIN® (bevacizumab), ABT-869, AEE-788, ANGIOZYME™ (a ribozyme that inhibits angiogenesis (Ribozyme Pharmaceuticals (Boulder, Colo.) and Chiron, (Emeryville, Calif.)), axitinib (AG-13736), AZD-2171, CP-547,632, IM-862, MACUGEN (pegaptamib), NEXAVAR® (sorafenib, BAY43-9006), pazopanib (GW-786034), vatalanib (PTK-787, ZK-222584), SUTENT® (sunitinib, SU-11248), VEGF trap, ZACTIMA™ (vandetanib, ZD-6474) and the like.

Antibiotics include intercalating antibiotics aclarubicin, actinomycin D, amrubicin, annamycin, adriamycin, BLENOXANE® (bleomycin), daunorubicin, CAELYX® or MYOCET® (liposomal doxorubicin), elsamitrucin, epirbucin, glarbuicin, ZAVEDOS® (idarubicin), mitomycin C, nemorubicin, neocarzinostatin, peplomycin, pirarubicin, rebeccamycin, stimalamer, streptozocin, VALSTAR® (vahrubicin), zinostatin and the like.

Topoisomerase inhibitors include aclarubicin, 9-aminocamptothecin, amonafide, amsacrine, becatecarin, belotecan, BN-80915, CAMPTOSAR® (irinotecan hydrochloride), camptothecin, CARDIOXANE® (dexrazoxine), diflomotecan, edotecarin, ELLENCE® or PHARMORUBICIN® (epirubicin), etoposide, exatecan, 10-hydroxycamptothecin, gimatecan, lurtotecan, mitoxantrone, orathecin, pirarbucin, pixantrone, rubitecan, sobuzoxane, SN-38, tafluposide, topotecan and the like.

Antibodies include AVASTIN® (bevacizumab), CD40-specific antibodies, chTNT-1/B, denosumab, ERBITUX® (cetuximab), HUMAX-CD4® (zanolimumab), IGF1R-specific antibodies, lintuzumab, PANOREX® (edrecolomab), RENCAREX® (WX G250), RITUXAN® (rituximab), ticilimumab, trastuzimab, CD20 antibodies types I and II and the like.

Hormonal therapies include ARIMIDEX® (anastrozole), AROMASIN® (exemestane), arzoxifene, CASODEX® (bicalutamide), CETROTIDE® (cetrorelix), degarelix, deslorelin, DESOPAN® (trilostane), dexamethasone, DROGENIL® (flutamide), EVISTA® (raloxifene), AFEMA™ (fadrozole), FARESTON® (toremifene), FASLODEX® (fulvestrant), FEMARA® (letrozole), formestane, glucocorticoids, HECTOROL® (doxercalciferol), RENAGEL® (sevelamer carbonate), lasofoxifene, leuprolide acetate, MEGACE® (megesterol), MIFEPREX® (mifepristone), NILANDRON™ (nilutamide), NOLVADEX® (tamoxifen citrate), PLENAXIS™ (abarelix), prednisone, PROPECIA® (finasteride), rilostane, SUPREFACT® (buserelin), TRELSTAR® (luteinizing hormone releasing hormone (LHRH)), VANTAS® (Histrelin implant), VETORYL® (trilostane or modrastane), ZOLADEX® (fosrelin, goserelin) and the like.

Deltoids and retinoids include seocalcitol (EB1089, CB1093), lexacalcitrol (KH1060), fenretinide, PANRETIN® (aliretinoin), ATRAGEN® (liposomal tretinoin), TARGRETIN® (bexarotene), LGD-1550 and the like.

PARP inhibitors include ABT-888 (veliparib), olaparib, KU-59436, AZD-2281, AG-014699, BSI-201, BGP-15, INO-1001, ONO-2231 and the like.

Plant alkaloids include, but are not limited to, vincristine, vinblastine, vindesine, vinorelbine and the like.

Proteasome inhibitors include VELCADE® (bortezomib), MG132, NPI-0052, PR-171 and the like.

Examples of immunologicals include interferons and other immune-enhancing agents. Interferons include interferon alpha, interferon alpha-2a, interferon alpha-2b, interferon beta, interferon gamma-1a, ACTIMMUNE® (interferon gamma-1b) or interferon gamma-n1, combinations thereof and the like. Other agents include ALFAFERONE®, (IFN-α), BAM-002 (oxidized glutathione), BEROMUN® (tasonermin), BEXXAR® (tositumomab), CAMPATH® (alemtuzumab), CTLA4 (cytotoxic lymphocyte antigen 4), decarbazine, denileukin, epratuzumab, GRANOCYTE® (lenograstim), lentinan, leukocyte alpha interferon, imiquimod, MDX-010 (anti-CTLA-4), melanoma vaccine, mitumomab, molgramostim, MYLOTARG™ (gemtuzumab ozogamicin), NEUPOGEN® (filgrastim), OncoVAC-CL, OVAREX® (oregovomab), pemtumomab (Y-muHMFG1), PROVENGE® (sipuleucel-T), sargaramostim, sizofilan, teceleukin, THERACYS® (Bacillus Calmette-Guerin), ubenimex, VIRULIZIN® (immunotherapeutic, Lorus Pharmaceuticals), Z-100 (Specific Substance of Maruyama (SSM)), WF-10 (Tetrachlorodecaoxide (TCDO)), PROLEUKIN® (aldesleukin), ZADAXIN® (thymalfasin), ZENAPAX® (daclizumab), ZEVALIN® (90Y-Ibritumomab tiuxetan) and the like.

Biological response modifiers are agents that modify defense mechanisms of living organisms or biological responses, such as survival, growth or differentiation of tissue cells to direct them to have anti-tumor activity and include krestin, lentinan, sizofiran, picibanil PF-3512676 (CpG-8954), ubenimex and the like.

Pyrimidine analogs include cytarabine (ara C or Arabinoside C), cytosine arabinoside, doxifluridine, FLUDARA® (fludarabine), 5-FU (5-fluorouracil), floxuridine, GEMZAR® (gemcitabine), TOMUDEX® (ratitrexed), TROXATYL™ (triacetyluridine troxacitabine) and the like.

Purine analogs include LANVIS® (thioguanine) and PURI-NETHOL® (mercaptopurine).

Antimitotic agents include batabulin, epothilone D (KOS-862), N-(24(4-hydroxyphenyl)amino)pyridin-3-yl)-4-methoxybenzenesulfonamide, ixabepilone (BMS 247550), paclitaxel, TAXOTERE® (docetaxel), PNU100940 (109881), patupilone, XRP-9881 (larotaxel), vinflunine, ZK-EPO (synthetic epothilone) and the like.

Ubiquitin ligase inhibitors include MDM2 inhibitors, such as nutlins, NEDD8 inhibitors such as MLN4924 and the like.

Compounds of this invention can also be used as radiosensitizers that enhance the efficacy of radiotherapy. Examples of radiotherapy include external beam radiotherapy, teletherapy, brachytherapy and sealed, unsealed source radiotherapy and the like.

Additionally, compounds having Formula (I) may be combined with other chemotherapeutic agents such as ABRAXANE™ (ABI-007), ABT-100 (farnesyl transferase inhibitor), ADVEXIN® (Ad5CMV-p53 vaccine), ALTOCOR® or MEVACOR® (lovastatin), AMPLIGEN® (poly I:poly C12U, a synthetic RNA), APTOSYN® (exisulind), AREDIA® (pamidronic acid), arglabin, L-asparaginase, atamestane (1-methyl-3,17-dione-androsta-1,4-diene), AVAGE® (tazarotene), AVE-8062 (combreastatin derivative) BEC2 (mitumomab), cachectin or cachexin (tumor necrosis factor), canvaxin (vaccine), CEAVAC® (cancer vaccine), CELEUK® (celmoleukin), CEPLENE® (histamine dihydrochloride), CERVARIX® (human papillomavirus vaccine), CHOP® (C: CYTOXAN® (cyclophosphamide); H: ADRIAMYCIN® (hydroxydoxorubicin); 0: Vincristine (ONCOVIN®); P: prednisone), CYPAT™ (cyproterone acetate), combrestatin A4P, DAB(389)EGF (catalytic and translocation domains of diphtheria toxin fused via a His-Ala linker to human epidermal growth factor) or TransMID-107R™ (diphtheria toxins), dacarbazine, dactinomycin, 5,6-dimethylxanthenone-4-acetic acid (DMXAA), eniluracil, EVIZON™ (squalamine lactate), DIMERICINE® (T4N5 liposome lotion), discodermolide, DX-8951f (exatecan mesylate), enzastaurin, EP0906 (epithilone B), GARDASIL® (quadrivalent human papillomavirus (Types 6, 11, 16, 18) recombinant vaccine), GASTRIMMUNE®, GENASENSE®, GMK (ganglioside conjugate vaccine), GVAX® (prostate cancer vaccine), halofuginone, histerelin, hydroxycarbamide, ibandronic acid, IGN-101, IL-13-PE38, IL-13-PE38QQR (cintredekin besudotox), IL-13-pseudomonas exotoxin, interferon-α, interferon-γ, JUNOVAN™ or MEPACT™ (mifamurtide), lonafarnib, 5,10-methylenetetrahydrofolate, miltefosine (hexadecylphosphocholine), NEOVASTAT®(AE-941), NEUTREXIN® (trimetrexate glucuronate), NIPENT® (pentostatin), ONCONASE® (a ribonuclease enzyme), ONCOPHAGE® (melanoma vaccine treatment), ONCOVAX® (IL-2 Vaccine), ORATHECIN™ (rubitecan), OSIDEM® (antibody-based cell drug), OVAREX® MAb (murine monoclonal antibody), paclitaxel, PANDIMEX™ (aglycone saponins from ginseng comprising 20(S)protopanaxadiol (aPPD) and 20(S)protopanaxatriol (aPPT)), panitumumab, PANVAC®-VF (investigational cancer vaccine), pegaspargase, PEG Interferon A, phenoxodiol, procarbazine, rebimastat, REMOVAB® (catumaxomab), REVLIMID® (lenalidomide), RSR¹³ (efaproxiral), SOMATULINE® LA (lanreotide), SORIATANE® (acitretin), staurosporine (Streptomyces staurospores), talabostat (PT100), TARGRETIN® (bexarotene), TAXOPREXIN® (DHA-paclitaxel), TELCYTA® (canfosfamide, TLK286), temilifene, TEMODAR® (temozolomide), tesmilifene, thalidomide, THERATOPE® (STn-KLH), thymitaq (2-amino-3,4-dihydro-6-methyl-4-oxo-5-(4-pyridylthio)quinazoline dihydrochloride), TNFERADE™ (adenovector: DNA carrier containing the gene for tumor necrosis factor-α), TRACLEER® or ZAVESCA® (bosentan), tretinoin (Retin-A), tetrandrine, TRISENOX® (arsenic trioxide), VIRULIZIN®, ukrain (derivative of alkaloids from the greater celandine plant), vitaxin (anti-alphavbeta3 antibody), XCYTRIN® (motexafin gadolinium), XINLAY™ (atrasentan), XYOTAX™ (paclitaxel poliglumex), YONDELIS® (trabectedin), ZD-6126, ZINECARD® (dexrazoxane), ZOMETA® (zolendronic acid), zorubicin and the like.

Data

Determination of the utility of compounds having Formula (I) as binders to and inhibitors of NAMPT was performed using a Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) binding assay.

Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Binding Assay of NAMPT

The assay was carried out in 18 uL low volume plates (Owens Corning) in reaction buffer (50 mM HEPES (NaOH), pH 7.5, 100 mM NaCl, 10 mM MgCl₂, 1 mM DTT, 1% Glycerol) using 6.8 nM recombinant, human, C-terminally-His tagged NAMPT, 1 nM Tb-anti-His antibody (Invitrogen, Cat # PV5895), and 200 nM probe (Oregon Green 488-conjugated AP0866; A-1251667.0 (probe 1) or A-1287128.0 (probe 2)). Plates were covered, and reactions were carried out for 2-3 hours. Plates were read with Envision (Laser Lantha low volume protocol) after 2 to 3 hours. Excitation was carried out at 337 nm, and the ratio of emission of Oregon Green (520 nm) to terbium (492 nm) was determined and used to calculate IC₅₀ values of test compounds.

TABLE 1 shows the utility of compounds having Formula I to functionally inhibit NAMPT.

TABLE 1 TR-FRET Binding IC50 (μM) Example probe 1, probe 2 1 0.0125, nd 2 0.00278, nd 3 0.00309, 0.00252 4 0.00371, nd 5 0.00692, 0.00832 6 0.00425, nd 7 0.0046, nd 8 0.00488, nd 9 0.00502, nd 10 0.00525, nd 11 0.00618, nd 12 0.00656, nd 13 0.00807, nd 14 0.00888, nd 15 0.00991, nd 16 0.0101, nd 17 0.0105, nd 18 0.011, nd 19 0.011, nd 20 0.011, nd 21 0.0112, nd 22 0.0116, nd 23 0.0119, nd 24 0.0123, nd 25 0.008, 0.00299 26 0.0126, nd 27 0.0138, nd 28 0.0141, nd 29 0.0145, nd 30 0.0146, nd 31 0.0149, nd 32 0.015, nd 33 0.015, nd 34 0.0151, nd 35 0.0152, nd 36 0.0157, nd 37 0.0161, nd 38 0.0164, nd 39 0.0166, nd 40 0.0171, nd 41 0.0174, nd 42 0.0174, 0.0173 43 0.0178, nd 44 0.018, nd 45 0.0181, nd 46 0.0183, nd 47 0.0185, nd 48 0.0186, nd 49 0.0186, nd 50 nd, nd 51 0.0191, nd 52 0.0197, nd 53 0.0197, nd 54 0.0201, nd 55 0.0202, nd 56 0.0203, nd 57 0.0211, nd 58 0.0212, nd 59 0.0229, 0.0154 60 0.0224, nd 61 0.0225, nd 62 0.0231, nd 63 0.0236, nd 64 0.0237, nd 65 0.0238, nd 66 0.024, nd 67 0.0241, nd 68 0.0247, nd 69 0.0248, nd 70 0.0248, nd 71 0.0256, nd 72 0.0258, nd 73 0.0267, nd 74 0.0273, nd 75 0.0274, nd 76 0.0278, nd 77 0.0284, nd 78 0.0293, nd 79 0.0295, nd 80 0.0299, nd 81 0.0301, nd 82 0.0301, nd 83 0.0306, nd 84 0.0308, nd 85 0.0313, nd 86 0.0319, nd 87 0.0326, nd 88 0.033, nd 89 0.0334, nd 90 0.0335, nd 91 0.0342, nd 92 0.0346, nd 93 0.0351, nd 94 0.0354, nd 95 nd, nd 96 0.0365, nd 97 0.037, nd 98 0.0381, nd 99 0.0382, nd 100 nd, nd 101 0.0393, nd 102 0.0395, nd 103 0.0395, nd 104 0.0395, nd 105 0.0397, nd 106 0.0263, nd 107 0.0408, nd 108 0.0408, nd 109 0.0412, nd 110 0.0422, nd 111 0.044, nd 112 0.0445, nd 113 0.0445, nd 114 0.0461, nd 115 0.0465, nd 116 0.0465, nd 117 0.0481, nd 118 0.0481, nd 119 0.0484, nd 120 0.049, nd 121 0.0493, nd 122 0.0511, nd 123 0.0515, nd 124 0.0517, nd 125 0.0518, nd 126 0.0537, nd 127 0.0539, nd 128 0.0553, nd 129 0.0567, nd 130 0.0567, nd 131 0.0573, nd 132 0.0581, nd 133 0.0582, nd 134 0.0613, nd 135 0.0615, nd 136 0.0616, nd 137 0.0629, nd 138 0.0632, nd 139 0.0638, nd 140 0.0655, nd 141 0.0656, nd 142 0.0664, nd 143 0.0665, nd 144 0.0666, nd 145 0.0692, nd 146 0.0694, nd 147 0.0701, nd 148 0.0702, nd 149 0.0717, nd 150 0.0728, nd 151 0.0733, nd 152 0.0759, nd 153 0.0799, nd 154 0.0813, nd 155 0.0834, nd 156 0.0836, nd 157 0.0846, nd 158 0.0857, nd 159 0.0858, nd 160 0.0861, nd 161 0.0876, nd 162 0.0882, nd 163 0.0893, nd 164 0.0907, nd 165 0.0931, nd 166 0.0999, nd 167 0.101, nd 168 0.105, nd 169 0.108, nd 170 0.108, nd 171 0.11, nd 172 0.111, nd 173 0.115, nd 174 0.12, nd 175 0.12, nd 176 0.12, nd 177 0.123, nd 178 nd, nd 179 0.128, nd 180 0.131, nd 181 0.133, nd 182 0.136, nd 183 0.14, nd 184 0.141, nd 185 0.142, nd 186 0.145, nd 187 0.146, nd 188 0.148, nd 189 0.149, nd 190 0.15, nd 191 0.154, nd 192 0.155, nd 193 0.164, nd 194 0.164, nd 195 0.172, nd 196 0.176, nd 197 0.178, nd 198 0.179, nd 199 0.179, nd 200 0.186, nd 201 0.189, nd 202 0.192, nd 203 0.198, nd 204 0.20, nd 205 0.203, nd 206 0.216, nd 207 0.219, nd 208 0.223, nd 209 0.146, 0.258 210 0.235, Nd 211 0.241, nd 212 0.252, nd 213 0.255, nd 214 0.265, nd 215 0.267, nd 216 0.271, nd 217 0.274, nd 218 0.279, nd 219 0.284, nd 220 0.293, nd 221 0.295, nd 222 0.297, nd 223 0.302, nd 224 0.317, nd 225 0.333, nd 226 0.339, nd 227 0.359, nd 228 0.359, nd 229 0.361, nd 230 0.369, nd 231 0.414, nd 232 0.42, nd 233 0.43, nd 234 0.43, nd 235 0.455, nd 236 0.457, nd 237 0.46, nd 238 0.504, nd 239 0.519, nd 240 0.52, nd 241 0.523, nd 242 0.524, nd 243 0.543, nd 244 0.574, nd 245 0.585, nd 246 0.618, nd 247 0.624, nd 248 0.738, nd 249 0.778, nd 250 0.78, nd 251 0.83, nd 252 0.837, nd 253 0.852, nd 254 0.877, nd 255 0.969, nd 256 1.23, nd 257 1.36, nd 258 1.52, nd 259 1.54, nd 260 1.57, 0.152 261 1.63, nd 262 1.66, nd 263 1.66, nd 264 1.92, nd 265 2.24, nd 266 2.29, nd 267 2.75, nd 268 2.85, nd 269 3.62, nd 270 4.7, nd 271 11.1, nd 272 0.0816, nd 273 1.0, nd 274 1.03, nd 275 0.197, nd 276 0.298, nd 277 1.02, nd 278 0.385, nd 279 1.91, nd 280 0.04453, 0.0612 281 0.0383, nd 282 0.14, nd 283 0.387, nd 284 0.0333, 0.0344 285 0.00192, 0.00259 286 0.00206, nd 287 0.00435, nd 288 0.00447, nd 289 0.00743, nd 290 0.0104, nd 291 0.0277, nd 292 0.0361, nd 293 0.00877, nd 294 0.00814, nd 295 0.0141, nd 296 0.0247, nd 297 0.012, nd 298 0.097, nd 299 0.00673, nd 300 0.0103, nd 301 0.0546, nd 302 0.0157, nd 303 0.251, nd 304 0.0133, nd 305 0.0121, nd 306 0.0133, nd 307 0.0254, nd 308 0.0808, nd 309 0.0634, nd 310 0.0368, nd 311 0.00524, nd 312 0.114, nd 313 0.00541, 0.00587 314 0.021, nd 315 0.00762, nd 316 0.287, nd 317 0.0421, nd 318 0.249, nd 319 0.0319, nd 320 0.272, nd 321 0.203, nd 322 0.0255, nd 323 0.0988, nd 324 0.333, nd 325 0.0987, nd 326 0.0743, nd 327 0.223, nd 328 0.331, nd 329 2.02, nd 330 0.00618, nd 331 0.00611, nd 332 0.0042, nd 333 0.00315, nd 334 0.0223, nd 335 0.00669, nd 336 0.0259, nd 337 0.0261, nd 338 0.0785, nd 339 0.315, nd 340 0.783, nd 341 0.101, nd 342 0.103, nd 343 0.0791, nd 344 0.216, nd 345 0.84, nd 346 0.0498, nd 347 0.297, nd 348 1.56, nd 349 0.0022, nd 350 0.00825, nd 351 0.064, nd 352 1.19, nd 353 0.00763, nd 354 0.0405, nd 355 0.124, nd 356 0.404, nd 357 9.88, nd 358 0.0711, nd 359 0.0881, nd 360 0.239, nd 361 0.436, nd 362 0.578, nd 363 2.04, nd 364 6.48, nd 365 11.2, nd 366 3.34, nd 367 4.84, nd 368 0.00373, nd 369 0.00656, nd 370 0.0075, nd 371 0.0395, nd 372 0.0535, nd 373 0.0234, nd 374 nd, nd 375 0.595, nd 376 nd, nd 377 0.105, nd 378 0.492, 0.377 379 0.0511, 0.0404 380 nd, 0.201 381 0.547, nd 382 0.257, nd 383 1.99, 1.34 384 0.00974, 0.00889 385 0.040, 0.0484 386 0.0707, nd 387 0.17, nd 388 5.7, 4.55 389 0.266, nd 390 0.727, 0.616 391 0.0465, 1.41 392 0.282, 0.288 393 0.415, 0.281 394 2.07, 1.45 395 1.84, 1.67 396 0.474, 0.278 397 0.405, 0.353 398 0.346, 0.272 399 0.0903, 0.0736 400 1.89, 2.35 401 0.072, nd 402 0.183, nd 403 0.606, nd 404 0.0277, nd 405 0.012, nd 406 0.011, nd 407 0.00145, nd 408 0.372, nd 409 1.02, nd 410 0.0295, nd 411 0.0197, nd 412 0.168, 0.109 413 2.01, nd 414 0.032, nd 415 0.0121, nd 416 0.041, nd 417 4.91, nd 418 0.506, 0.0514 419 0.010, nd 420 0.0182, nd 421 0.0404, nd 422 3.94, nd 423 12.5, nd 424 0.0826, nd 425 0.0814, nd 426 0.0104, nd 427 0.0154, nd 428 0.0327, nd 429 0.179, nd 430 0.191, nd 431 0.0607, nd 432 0.00874, nd 433 0.00807, nd 434 0.0507, nd 435 0.00589, nd 436 0.00933, nd 437 0.0080, nd 438 0.60, nd 439 1.69, nd 440 0.0355, nd 441 0.0237, 0.015 442 0.0492, nd 443 0.365, nd 444 0.281, nd 445 0.0141, nd 446 0.011, nd 447 0.0466, nd 448 0.021, nd 449 0.0257, nd 450 1.03, nd 451 0.000946, 0.00124 452 0.0512, nd 453 0.0527, nd 454 0.0803, nd 455 12.2, nd 456 0.0598, 0.0475 457 0.0756, nd 458 nd, nd 459 0.00362, nd 460 0.0193, nd 461 nd, 0.00815 462 0.00694, nd 463 0.0215, 0.013 464 0.0166, 0.0272 465 0.00823, 0.0238 466 nd, nd 467 0.0165, 0.047 468 0.00339, 0.00726 469 0.00597, 0.00947 470 0.00445, 0.0080 471 0.00811, 0.019 472 0.0149, 0.0107 473 0.00321, 0.00381 474 0.00389, 0.00775 475 0.0090, 0.0139 476 0.0125, 0.0468 477 0.00996, nd 478 0.015, 0.386 479 nd, 0.00399 480 0.00571, 0.0676 481 nd, nd 482 0.00511, nd 483 0.00479, 0.00937 484 nd, nd 485 0.00557, 0.0118 486 0.0047, 0.00497 487 0.00884, 0.0573 488 0.00825, 0.0211 489 0.0123, nd 490 0.0212, 0.028 491 0.00455, 0.0113 492 0.0396, 0.0417 493 0.0336, 0.013 494 0.016, 0.021 495 0.0516, 0.0607 496 0.0139, 0.0257 497 0.00331, 0.0048 498 0.307, nd 499 0.806, nd 500 0.182, nd 501 0.0459, 0.018 502 0.157, nd 503 0.0786, nd 504 0.0766, 0.0563 505 0.0204, 0.0182 506 0.0332, 0.0227 507 0.186, nd 508 0.184, nd 509 0.211, nd 510 0.0337, 0.0221 511 0.0176, 0.0275 512 0.0436, 0.0443 513 0.0539, 0.0681 514 0.0481, 0.0673 515 0.0723, 0.0666 516 0.0106, 0.00847 517 0.0758, nd 518 0.266, nd 519 0.0968, nd 520 0.0488, nd 521 0.0601, 0.0631 522 0.0296, 0.0611 523 0.187, nd 524 0.115, nd 525 0.0375, 0.060 526 0.076, 0.0644 527 0.0168, 0.0243 528 0.0521, 0.0454 529 0.103, nd 530 0.124, nd 531 0.159, nd 532 0.488, nd 533 0.294, nd 534 0.14, nd 535 0.743, nd 536 0.187, nd 537 0.0132, 0.0106 538 0.072, 0.0829 539 0.072, 0.0417 540 0.137, nd 541 0.225, nd 542 0.00277, 0.0026 543 0.00213, 0.00302 544 0.00302, 0.00305 545 0.00278, 0.0020 546 0.00332, 0.00322 547 nd, nd 548 nd, nd 549 nd, nd 550 nd, nd 551 nd, nd 552 nd, nd 553 0.00755, 0.00582 554 0.00401, 0.00519 555 0.0196, 0.0114 556 0.0145, 0.0102 557 0.862, 1.98 558 1.84, 5.63 559 1.98, nd 560 5.02, nd 561 0.268, nd 562 0.0189, 0.0177 563 0.00166, 0.00361 564 0.00196, 0.00159 565 0.0083, 0.00737 566 0.193, nd 567 0.00675, 0.00624 568 0.00412, 0.00501 569 0.00808, 0.0085 570 0.00913, 0.00995 571 0.0138, 0.0104 572 0.00845, 0.00972 573 1.26, nd 574 0.0794, 0.0621 575 0.0538, 0.0378 576 0.0902, 0.0507 577 0.00439, 0.00297 578 0.060, 0.0707 579 0.00314, 0.00247 580 0.00239, 0.00201 581 0.0040, 0.00338 582 0.00205, 0.00169 583 0.00282, 0.0027 584 0.0147, 0.0117 585 nd, 0.0271 586 nd, 0.0338 587 nd, 0.444 588 nd, 0.739 589 nd, 0.044 590 nd, 0.0428 591 nd, 0.661 592 nd, 0.0884 593 nd, 0.0269 594 nd, 0.021 595 nd, 0.0651 596 nd, 0.00448 597 nd, 0.0631 598 nd, 0.0322 599 nd, 0.0582 600 nd, 0.0385 601 nd, 0.0326 602 nd, 0.0392 603 nd, 0.056 604 nd, 0.0224 605 nd, 0.00759 606 nd, 0.0139 607 nd, 0.00159 608 nd, 0.00985 609 nd, 0.196 610 nd, 1.3 611 nd, 0.328 612 nd, 0.365 613 nd, 0.119 614 nd, 0.0482 615 nd, 0.0842 616 nd, 0.097 617 nd, 1.13 618 nd, 0.00755 619 nd, 0.0827 620 nd, 0.00755 621 nd, 0.0118 622 nd, 0.0595 623 nd, 1.48 624 nd, 0.046 625 nd, 0.0107 626 nd, 0.00759 627 nd, 0.164 628 nd, 0.0234 629 nd, 0.0335 630 nd, 0.0725 631 nd, 0.0506 632 nd, 0.104 633 nd, 0.0873 634 nd, 0.0361 635 nd, 0.129 636 nd, 1.21 637 nd, 0.0542 638 nd, 0.102 639 nd, 0.0882 640 nd, 0.135 641 nd, 0.163 642 nd, 0.507 643 nd, 0.0633 644 nd, 0.0594 645 nd, 0.125 646 nd, 0.00568 647 nd, 0.0385 648 nd, 0.845 649 nd, 0.0445 650 nd, 0.106 651 nd, 0.0207 652 nd, 0.00488 653 nd, 0.0144 654 nd, 0.0256 655 nd, 0.0224 656 nd, 0.116 657 nd, 0.0533 658 nd, 0.00549 659 nd, 0.00585 660 nd, 0.0221 661 nd, 0.00253 662 nd, 0.00977 663 nd, 0.0136 664 nd, 0.00412 665 nd, 0.00814 666 nd, 0.0111 667 nd, 0.00905 668 nd, 0.00698 669 nd, 0.0136 670 nd, 0.0183 671 nd, 0.0238 672 nd, 0.011 673 nd, 0.0248 674 nd, 0.00839 675 nd, 0.0414 676 nd, 0.0165 677 nd, 0.0126 678 nd, 0.00265 679 nd, 0.00461 680 nd, 0.126 681 nd, 0.0603 682 nd, 0.019 683 nd, 0.0669 684 nd, 0.0153 685 nd, 0.0205 686 nd, 0.653 687 nd, 0.0238 688 nd, 0.00303 689 nd, 0.0123 690 nd, 0.00616 691 nd, 0.0392 692 nd, 0.0247 693 nd, 0.0264 694 nd, 0.0359 695 nd, 0.027 696 nd, 0.00223 697 nd, 0.0049 698 nd, 0.0327 699 nd, 0.00558 700 nd, 0.0204 701 nd, 0.0227 702 nd, 0.0232 703 nd, 0.0829 704 nd, 0.0126 705 nd, 0.00742 706 nd, 0.00581 707 nd, 0.00573 708 nd, 0.00997 709 nd, 0.00601 710 nd, 0.00336 711 nd, 0.0462 712 nd, 0.0453 713 nd, 0.0529 714 nd, 0.121 715 nd, 0.136 716 nd, 0.102 717 nd, 0.0718 718 nd, 0.012 719 nd, 0.0347 720 nd, 0.164 721 nd, 0.14 722 nd, 0.00157 723 nd, 0.0209 724 nd, 0.0851 725 nd, 0.477 726 nd, 0.577 727 nd, 1.22 728 nd, 0.00752 729 nd, 0.0445 730 nd, 0.45 731 nd, 0.0183 732 nd, 0.0241 733 nd, 0.0598 734 nd, 0.0845 735 nd, 0.126 736 nd, 0.281 737 nd, 0.186 738 nd, 0.00417 739 nd, 0.0049 740 nd, 0.204 741 nd, 0.0165 742 nd, 0.0331 743 nd, 0.00971 744 nd, 0.00446 745 nd, 0.00868 746 nd, 0.0768 747 nd, 0.00434 748 nd, 0.00455 749 nd, 0.0161 750 nd, 0.0118 751 nd, 0.229 752 nd, 0.0108 753 nd, 0.0655 754 nd, 0.0683 755 nd, 0.0407 756 nd, 0.0488 757 nd, 0.00201 758 nd, 0.0293 759 nd, 0.00581 760 nd, 0.00483 761 nd, 0.0131 762 nd, 0.0173 763 nd, 0.00528 764 nd, 0.0581 765 nd, 0.0532 766 nd, 0.0468 767 nd, 0.169 768 nd, 0.13 769 nd, 0.0695 770 nd, 0.135 771 nd, 0.0893 772 nd, 0.0534 773 nd, 0.297 774 nd, 0.0826 775 nd, 0.0951 776 nd, 0.00746 777 nd, 0.00625 778 nd, 0.0259 779 nd, 0.0385 780 nd, 0.109 781 nd, 0.0158 782 nd, 0.0296 783 nd, 0.029 784 nd, 0.0224 785 nd, 0.0262 786 nd, 0.0262 787 nd, 0.13 788 nd, 0.0785 789 nd, 0.00318 790 nd, 0.159 791 nd, 0.00977 792 nd, 0.0217 793 nd, 0.0118 794 nd, 0.017 795 nd, 0.991 796 nd, 0.00322 797 nd, 0.00295 798 nd, 0.00221 799 nd, 0.00361 800 nd, 0.0821 801 nd, 0.30 802 nd, 0.0258 803 nd, 0.0132 804 nd, 0.0373 805 nd, 0.0287 806 nd, 0.286 807 nd, 0.0417 808 nd, 0.696 809 nd, 0.00207 810 nd, nd 811 nd, 0.00359 812 nd, 0.00679 813 nd, 0.0446 814 nd, 0.00713 815 nd, 0.00287 816 nd, 0.0243 817 nd, 0.00251 818 nd, 0.0128 819 nd, 0.00428 820 nd, 0.00631 821 nd, 0.012 822 nd, 0.00207 823 nd, 0.00176 824 nd, 0.0066 825 nd, 0.0107 826 nd, 0.00918 827 nd, 0.00311 828 nd, 0.00737 829 nd, 0.00359 830 nd, nd 831 nd, 0.00918 832 nd, 0.00888 833 nd, 0.0034 834 nd, 0.00358 835 nd, 0.00353 836 nd, 0.00454 837 nd, 0.00367 838 nd, 0.00203 839 nd, 0.0191 840 nd, 0.725 841 nd, 1.61 842 nd, 0.0746 843 nd, 0.704 844 nd, 2.62 845 nd, 5.64 846 nd, 2.99 847 nd, 0.24 848 nd, 1.19 849 nd, 5.71 850 nd, 2.1 851 nd, 0.277 852 nd, 5.48 853 nd, 12.5 854 nd, 5.66 855 nd, 0.839 856 nd, 0.00913 857 nd, 0.061 858 nd, 0.0082 859 nd, 2.14 860 nd, 12.5 861 nd, 3.15 862 nd, 0.599 863 nd, 0.143 864 nd, 0.122 865 nd, 1.56 866 nd, 0.14 867 nd, 0.0593 868 nd, 0.128 869 nd, 0.229 870 nd, 0.12 871 nd, 0.036 872 nd, 0.00746 873 nd, 0.00465 874 nd, 0.00231 875 nd, 0.00419 876 nd, 0.0022 877 nd, 0.00882 878 nd, 0.0525 879 nd, 0.00298 880 nd, 0.0517 881 nd, 0.0463 882 nd, 0.0377 883 nd, 0.0156 884 nd, 0.0154 885 nd, 0.466 886 nd, 0.0246 887 nd, 0.826 888 nd, 0.0934 889 nd, 1.47 890 nd, 1.38 891 nd, 1.72 892 nd, 1.84 893 nd, 0.154 894 nd, 0.00302 895 nd, 0.0261 896 nd, 0.444 897 nd, 0.969 898 nd, 0.288 899 nd, 0.19 900 nd, 0.0437 901 nd, 0.0676 902 nd, 0.35 903 nd, 0.0491 904 nd, 0.0351 905 nd, 0.0383 906 nd, 0.0569 907 nd, 0.0711 908 nd, 0.0334 909 nd, 0.0019 910 nd, 0.00638 911 nd, 0.0133 912 nd, 0.00832 913 nd, 0.0074 914 nd, 0.00486 915 nd, 0.0188 916 nd, 0.0221 917 nd, 0.00207 918 nd, 0.0128 919 nd, 0.00708 920 nd, 0.548 921 nd, 0.0602 922 nd, 0.00567 923 nd, 0.00395 924 nd, 0.00277 925 nd, 0.00683 926 nd, 0.0508 927 nd, 0.0406 928 nd, 0.0725 929 nd, 0.21 930 nd, 0.146 931 nd, 0.0981 932 nd, 1.31 933 nd, 0.206 934 nd, 0.00168 935 nd, 0.00584 936 nd, 0.121 937 nd, 0.0398 938 nd, 0.0877 939 nd, 0.0105 940 nd, 0.0168 941 nd, 0.136 942 nd, 0.0238 943 nd, 0.0090 944 nd, 0.0328 945 nd, 0.0433 946 nd, 0.0172 947 nd, 0.0459 948 nd, 0.0192 949 nd, 0.0309 950 nd, 0.0198 951 nd, 0.00968 952 nd, 0.0128 953 nd, 0.426 954 nd, 0.341 955 nd, 0.222 956 nd, 0.346 957 nd, 0.374 958 nd, 0.148 959 nd, 0.307 960 nd, 0.22 961 nd, 0.161 962 nd, 0.201 963 nd, 0.198 964 nd, 0.128 965 nd, 0.17 966 nd, 0.223 967 nd, 0.0047 968 nd, 0.00259 969 nd, 0.0234 970 nd, 0.0213 971 nd, 0.0205 972 nd, 0.00919 973 nd, 0.0435 974 nd, 0.034 975 nd, 0.0115 976 nd, 0.0225 977 nd, 0.0214 978 nd, 0.0236 979 nd, 0.0365 980 nd, 0.0173 981 nd, 0.034 982 nd, 0.0144 983 nd, 0.0296 984 nd, 0.0689 985 nd, 0.00963 986 nd, 0.0407 987 nd, 0.111 988 nd, nd 989 nd, 0.0269 990 nd, 0.031 991 nd, 0.0408 992 nd, 0.0168 993 nd, 0.00941 994 nd, 0.00802 995 nd, 0.0285 996 nd, 0.101 997 nd, 0.175 998 nd, 0.0277 999 nd, 0.0166 1000 nd, 0.0391 1001 nd, 0.00157 1002 nd, 0.0426 1003 nd, 0.0489 1004 nd, 0.0461 1005 nd, 0.0385 1006 nd, 0.0252 1007 nd, 0.0598 1008 nd, 0.0349 1009 nd, 0.0266 1010 nd, 0.114 1011 nd, 0.0264 1012 nd, 0.0923 1013 nd, 0.389 1014 nd, 0.00661 1015 nd, 0.00631 1016 nd, 0.00375 1017 nd, 0.00201 1018 nd, 0.0244 1019 nd, 0.00144 1020 nd, 10.0 1021 nd, 1.17 1022 nd, 0.0135 1023 nd, 0.0127 1024 nd, 0.0921 1025 nd, 0.00795 1026 nd, 0.035 1027 nd, 0.0842 1028 nd, 0.0519 1029 nd, 0.035 1030 nd, 0.0116 1031 nd, 0.0251 1032 nd, 0.156 1033 nd, 0.113 1034 nd, 0.164 1035 nd, 0.376 1036 nd, 0.20 1037 nd, 0.048 1038 nd, 0.0248 1039 nd, 0.105 1040 nd, 0.0163 1041 nd, 0.0128 1042 nd, 0.00968 1043 nd, 0.00489 1044 nd, 0.00621 1045 nd, 0.00924 1046 nd, 0.0469 1047 nd, 0.0542 1048 nd, 0.0345 1049 nd, 0.0398 1050 nd, 0.102 1051 nd, 0.0626 1052 nd, 0.0318 1053 nd, 0.0764 1054 nd, 0.0563 1055 nd, 1.55 1056 nd, 0.335 1057 nd, 2.32 1058 nd, 1.12 1059 nd, 0.394 1060 nd, 1.57 1061 nd, 1.78 1062 nd, 0.222 1063 nd, 0.00988 1064 nd, 0.0621 1065 nd, 0.00445 1066 nd, 0.318 1067 nd, 0.738 1068 nd, 0.365 1069 nd, 0.122 1070 nd, 0.332 1071 nd, 0.993 1072 nd, 0.117 1073 nd, 0.0659 1074 nd, 0.0674 1075 nd, 0.0931 1076 nd, 0.0389 1077 nd, 0.0069 1078 nd, 0.00347 1079 nd, 0.0259 1080 nd, 0.00297 1081 nd, 0.00682 1082 nd, 0.0195 1083 nd, 0.0117 1084 nd, 0.0296 1085 nd, 0.029 1086 nd, 0.0152 1087 nd, 0.00733 1088 nd, 0.0155 1089 nd, 0.0771 1090 nd, 0.0493 1091 nd, 0.0289 1092 nd, 0.0192 1093 nd, 0.0117 1094 nd, 0.044 1095 nd, 0.0118 1096 nd, 0.028 1097 nd, 0.0756 1098 nd, 0.0111 1099 nd, 0.145 1100 nd, 0.0263 1101 nd, 0.0448 1102 nd, 0.108 1103 nd, 0.00784 1104 nd, 1.69 1105 nd, 0.0619 1106 nd, 0.364 1107 nd, 0.152 1108 nd, 0.0061 1109 nd, 0.048 1110 nd, 0.0151 1111 nd, 0.0139 1112 nd, 0.0498 1113 nd, 0.00326 1114 nd, 0.0281 1115 nd, 0.0188 1116 nd, 0.0419 1117 nd, 0.0332 1118 nd, 0.00548 1119 nd, 0.0224 1120 nd, 0.0227 1121 nd, 0.0302 1122 nd, 0.162 1123 nd, 0.0309 1124 nd, 0.0143 1125 nd, 0.0764 1126 nd, 0.311 1127 nd, 0.00569 1128 nd, 0.199 1129 nd, 0.546 1130 nd, 0.0354 1131 nd, 0.0414 1132 nd, 0.201 1133 nd, 0.703 1134 nd, 0.175 1135 nd, 0.121 1136 nd, 0.0498 1137 nd, 0.0119 1138 nd, 0.0874 1139 nd, 0.333 1140 nd, 0.138 1141 nd, 0.0099 1142 nd, 0.136 1143 nd, 0.328 1144 nd, 0.00515 1145 nd, 0.00619 1146 nd, 0.0148 1147 nd, 0.00824 1148 nd, 0.0409 1149 nd, 0.0824 1150 nd, 0.0132 1151 nd, 0.048 1152 nd, 0.233 1153 nd, 0.00492 1154 nd, 0.00962 1155 nd, 0.033 1156 nd, 0.216 1157 nd, 0.0725 1158 nd, 0.0125 1159 nd, 0.0179 1160 nd, 0.237 1161 nd, 0.0044 1162 nd, 0.00954 1163 nd, 0.0174 1164 nd, 0.00544 1165 nd, nd 1166 nd, 0.0562 1167 nd, 0.0298 1168 nd, nd 1169 nd, 0.239 1170 nd, 0.0214 1171 nd, 0.0105 1172 nd, 0.00867 1173 nd, 0.0437 1174 nd, 0.0156 1175 nd, 0.00662 1176 nd, 0.00915 1177 nd, 0.0496 1178 nd, 0.112 1179 nd, 0.0791 1180 nd, 0.0102 1181 nd, 0.128 1182 nd, nd 1183 nd, 0.0404 1184 nd, 0.109 1185 nd, 0.0503 1186 nd, 0.0106 1187 nd, 0.00878 1188 nd, 0.00494 1189 nd, 0.0291 1190 nd, 0.0843 1191 nd, 0.0607 1192 nd, 0.17 1193 nd, 0.00776 1194 nd, 0.171 1195 nd, 0.0205 1196 nd, 0.0102 1197 nd, 0.101 1198 nd, nd 1199 nd, 0.165 1200 nd, nd 1201 nd, 0.0422 1202 nd, 0.0227 1203 nd, 0.378 1204 nd, 0.0772 1205 nd, 0.345 1206 nd, 0.394 1207 nd, 0.283 1208 nd, 0.028 1209 nd, 0.0387 1210 nd, 0.0192 1211 nd, 0.879 1212 nd, 0.144 1213 nd, nd 1214 nd, 0.035 1215 nd, 0.133 1216 nd, 0.054 1217 nd, 0.0316 1218 nd, 0.158 1219 nd, 0.0613 1220 nd, 0.0181 1221 nd, 1.13 1222 nd, 0.0513 1223 nd, 0.0192 1224 nd, 0.497 1225 nd, 0.0767 1226 nd, 0.0116 1227 nd, 0.0534 1228 nd, 0.418 1229 nd, 0.393 1230 nd, 0.0674 1231 nd, 0.576 1232 nd, 0.0248 1233 nd, 0.351 1234 nd, 0.0174 1235 nd, 0.0668 1236 nd, 0.078 1237 nd, 0.561 1238 nd, 0.748 1239 nd, 0.328 1240 nd, 0.592 1241 nd, 0.0122 1242 nd, 0.0488 1243 nd, 0.142 1244 nd, 2.23 1245 nd, 0.0214 1246 nd, 0.803 1247 nd, 0.212 1248 nd, 0.373 1249 nd, 0.17 1250 nd, 0.335 1251 nd, 0.111 1252 nd, 0.125 1253 nd, 0.669 1254 nd, 0.00222 1255 nd, 0.00211 1256 nd, 0.00328 1257 nd, 0.00482 1258 nd, 0.00831 1259 nd, 0.00191 1260 nd, 0.00491 1261 nd, 0.0583 1262 nd, 0.109 1263 nd, 0.0116 1264 nd, 0.309 1265 nd, 0.0393 1266 nd, 0.113 1267 nd, 0.285 1268 nd, 0.932 1269 nd, 0.216 1270 nd, 0.0109 1271 nd, 0.0627 1272 nd, 0.0224 1273 nd, 0.132 1274 nd, 0.199 1275 nd, 0.097 1276 nd, 0.0269 1277 nd, 0.0429 1278 nd, 0.0136 1279 nd, 0.00784 1280 nd, 0.00438 1281 nd, 0.00122 1282 nd, 0.00134 1283 nd, 0.00151 1284 nd, 0.00172 1285 nd, 0.0432 1286 nd, 0.00323 1287 nd, 0.00325 1288 nd, 0.0228 1289 nd, 0.0267 1290 nd, 0.409 1291 nd, 0.00847 1292 nd, 0.0252 1293 nd, 0.0165 1294 nd, 0.0327 1295 nd, 0.0607 1296 nd, 0.0175 1297 nd, 0.0238 1298 nd, 0.032 1299 nd, 0.0424 1300 nd, 0.0111 1301 nd, 0.0197 1302 nd, 0.0734 1303 nd, 0.209 1304 nd, 0.204 1305 nd, 0.431 1306 nd, 0.224 1307 nd, 0.401 1308 nd, 0.139 1309 nd, 0.0767 1310 nd, nd 1311 nd, 0.0917 1312 nd, 0.0265 1313 nd, 0.0783 1314 nd, 0.0247 1315 nd, 0.214 1316 nd, 0.379 1317 nd, 0.074 1318 nd, 0.0456 1319 nd, 0.0147 1320 nd, 0.0163 1321 nd, 0.0148 1322 nd, nd 1323 nd, nd 1324 nd, 0.0779 1325 nd, 0.0903 1326 nd, 0.0216 1327 nd, 1.46 1328 nd, 0.147 1329 nd, 0.0143 1330 nd, 0.0179 1331 nd, 0.206 1332 nd, 0.0414 1333 nd, 0.0195 1334 nd, nd 1335 nd, 0.0855 1336 nd, 0.0746 1337 nd, 0.105 1338 nd, 0.0244 1339 nd, 0.0202 1340 nd, 0.257 1341 nd, 0.195 1342 nd, 0.0269 1343 nd, 0.0114 1344 nd, 0.0821 1345 nd, 0.183 1346 nd, 0.275 1347 nd, 0.0292 1348 nd, 0.0565 1349 nd, 0.029 1350 nd, 0.0149 1351 nd, 0.0184 1352 nd, 0.0113 1353 nd, 0.00584 1354 nd, 0.00438 1355 nd, 0.00307 1356 nd, 0.00784 1357 nd, 0.0082 1358 nd, 0.013 1359 nd, 0.0129 1360 nd, 0.00654 1361 nd, 0.00515 1362 nd, 0.0055 1363 nd, 0.00534 1364 nd, 0.0149 1365 nd, 0.0119 1366 nd, 0.0476 1367 nd, 0.0291 1368 nd, 0.0151 1369 nd, 0.056 1370 nd, 0.00237 1371 nd, 0.0176 1372 nd, 0.0106 1373 nd, 0.0937 1374 nd, nd 1375 nd, 0.436 1376 nd, 0.381 1377 nd, 0.275 1378 nd, nd 1379 nd, 0.0867 1380 nd, 0.0936 1381 nd, 0.189 1382 nd, 0.237 1383 nd, 0.225 1384 nd, 0.0123 1385 nd, 0.00676 1386 nd, 0.0815 1387 nd, 0.0275 1388 nd, 0.00403 1389 nd, 0.00592 1390 nd, 0.0148 1391 nd, 0.00956 1392 nd, nd 1393 nd, 0.0129 1394 nd, nd 1395 nd, 0.0176 1396 nd, 0.00585 1397 nd, nd 1398 nd, 0.0559 1399 nd, 0.179 1400 nd, 0.0241 1401 nd, 0.018 1402 nd, 0.0412 1403 nd, 0.0322 1404 nd, 0.0561 1405 nd, 0.127 1406 nd, 0.194 1407 nd, 0.227 1408 nd, 0.222 1409 nd, 0.0823 1410 nd, 0.0722 1411 nd, 0.135 1412 nd, nd 1413 nd, 0.364 1414 nd, 0.00826 1415 nd, 0.0111 1416 nd, 0.00622 1417 nd, 0.0125 1418 nd, 0.0113 1419 nd, 0.0116 1420 nd, nd 1421 nd, 0.00753 1422 nd, 0.0069 1423 nd, 0.00831 1424 nd, 0.0135 1425 nd, 0.035 1426 nd, 0.0267 1427 nd, 0.033 1428 nd, 0.0184 1429 nd, 0.0069 1430 nd, 0.266 1431 nd, 0.011 1432 nd, nd 1433 nd, 0.0587 1434 nd, 0.0574 1435 nd, 0.0266 1436 nd, 0.0484 1437 nd, 0.0738 1438 nd, 0.0276 1439 nd, nd 1440 nd, nd 1441 nd, 0.032 1442 nd, 0.0136 1443 nd, 0.0148 1444 nd, 0.00577 1445 nd, 0.0128 1446 nd, 0.0113 1447 nd, 0.0105 1448 nd, 0.0223 1449 nd, 0.0186 1450 nd, 0.0154 1451 nd, 0.0139 1452 nd, 0.00765 1453 nd, 0.0617 1454 nd, 0.0678 1455 nd, 0.124 1456 nd, 0.0422 1457 nd, 0.0715 1458 nd, 0.0764 1459 nd, 0.0669 1460 nd, 0.126 1461 nd, 0.0487 1462 nd, 0.0694 1463 nd, 0.0779 1464 nd, 0.109 1465 nd, 0.101 1466 nd, 0.0125 1467 nd, 0.0164 1468 nd, 0.00486 1469 nd, 0.0138 1470 nd, 0.00221 1471 nd, 0.0109 1472 nd, 0.0125 1473 nd, 0.00872 1474 nd, 0.00888 1475 nd, 0.00744 1476 nd, 0.21 1477 nd, 0.0452 1478 nd, 0.0682 1479 nd, 0.0015 1480 nd, 0.00425 1481 nd, 0.00416 1482 nd, 0.00488 1483 nd, nd 1484 nd, 0.00149 1485 nd, 0.00323 1486 nd, 0.00137 1487 nd, 0.00234 1488 nd, 0.00844 1489 nd, 0.00656 1490 nd, nd 1491 nd, nd 1492 nd, 0.00153 1493 nd, 0.00295 1494 nd, 0.00202 1495 nd, 0.00877 1496 nd, 0.00844 1497 nd, 0.00135 1498 nd, 0.00228 1499 nd, 0.00152 1500 nd, 0.00415 1501 nd, 0.00264 1502 nd, 0.0101 1503 nd, 0.0067 1504 nd, 0.0101 1505 nd, nd 1506 nd, 0.00219 1507 nd, nd 1508 nd, 0.00244 1509 nd, 0.00397 1510 nd, 0.00326 1511 nd, 0.00664 1512 nd, nd 1513 nd, 0.0028 1514 nd, 0.00183 1515 nd, 0.00159 1516 nd, 0.00457 1517 nd, 0.00103 1518 nd, 0.00155 1519 nd, 0.00168 1520 nd, 0.00203 1521 nd, 0.0019 1522 nd, 0.0316 1523 nd, 0.0134 1524 nd, 0.00324 1525 nd, 0.0063 1526 nd, 0.00714 1527 nd, 0.0026 1528 nd, 0.00881 1529 nd, 0.00174 1530 nd, 0.00389 1531 nd, 0.124 1532 nd, 0.00541 1533 nd, 0.0102 1534 nd, 0.0213 1535 nd, 0.0201 1536 nd, 0.0114 1537 nd, 0.0118 1538 nd, 0.0257 1539 nd, 0.0611 1540 nd, 0.0644 1541 nd, 0.031 1542 nd, 0.762 1543 nd, 0.20 1544 nd, 0.193 1545 nd, 0.774 1546 nd, 0.0241 1547 nd, 0.00501 1548 nd, 0.000973 1549 nd, 0.00471 1550 nd, 0.0112 1551 nd, 0.00472 1552 nd, 0.00086 1553 nd, 0.0216 1554 nd, 0.0385 1555 nd, 0.0104 1556 nd, 0.0488 1557 nd, 0.0058 1558 nd, 0.0165 1559 nd, 0.0447 1560 nd, 0.0655 nd = not determined

ROCK2 Kinase Activity Assays

[³³P]-ATP Assay:

ROCK2 activity was initially determined using a radioactive FlashPlate-based assay. In a 96-well format, biotinylated peptide substrates (2 μM final; S6-short for ROCK2), γ-[³³P]-ATP (5 μM, 2 mCi/μmol), compounds (0.1-10000 nM in 2% DMSO), and ROCK2 (0.2 nM; Upstate) catalytic domains.

HTRF Assay:

This assay used the CisBio HTRF KinEASE kit (kit 62ST2PEZ) and the kinase reaction containing 0.2 μM biotinylated substrate peptide (S2, CisBio), 5 μM, 100 μM or 1 mM of ATP, inhibitors (0.1-10,000 nM in 2% DMSO) and enzymes as in the ³³P-ATP assay above.

TABLE 2 shows the results of the HTRF assay and the utility of compounds having Formula I to functionally inhibit ROCK2.

TABLE 2 ROCK2 HTRF Binding Example Ki (μM) 374 0.0036 375 4.06 376 0.00526 377 0.0195 378 0.00237 379 0.0024 380 0.0023 381 0.00412 382 0.00614 383 0.00361 384 0.00424 385 0.00651 386 10 387 0.00139 388 0.0112 389 0.00174 390 0.00245 391 0.00049 392 nd 393 nd 394 0.0093 395 0.0321 396 0.182 397 0.138 398 0.0022 399 nd 400 0.0251 547 0.179 548 0.014 549 0.0031 550 0.0154 551 0.0184 552 3.27 nd = not determined

Compounds which inhibit NAMPT are useful for treating diseases in which activation of NF-KB is implicated. Such methods are useful in the treatment of a variety of diseases including inflammatory and tissue repair disorders; particularly rheumatoid arthritis, inflammatory bowel disease, asthma and COPD (chronic obstructive pulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases; dermatosis, including psoriasis, atopic dermatitis and ultra-violet induced skin damage; autoimmune diseases including systemic lupus erythematosis, multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, particularly wherein the cancer is selected from breast, prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas, leukaemia, lymphoma or Hodgkin's disease, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, and ataxia telengiectasia.

Involvement of NAMPT in the treatment of cancer is described in WO 97/48696. Involvement of NAMPT in immuno-supression is described in WO 97/48397. Involvement of NAMPT for the treatment of diseases involving angiogenesis is described in WO 2003/80054. Involvement of NAMPT for the treatment of rheumatoid arthritis and septic shock is described in WO 2008/025857. Involvement of NAMPT for the prophlaxis and treatment of ischaemia is described in WO 2009/109610.

Cancers include, but are not limited to, hematologic and solid tumor types such as acoustic neuroma, acute leukemia, acute lymphoblastic leukemia, acute myelogenous leukemia (monocytic, myeloblastic, adenocarcinoma, angiosarcoma, astrocytoma, myelomonocytic and promyelocytic), acute t-cell leukemia, basal cell carcinoma, bile duct carcinoma, bladder cancer, brain cancer, breast cancer (including estrogen-receptor positive breast cancer), bronchogenic carcinoma, Burkitt's lymphoma, cervical cancer, chondrosarcoma, chordoma, choriocarcinoma, chronic leukemia, chronic lymphocytic leukemia, chronic myelocytic (granulocytic) leukemia, chronic myelogenous leukemia, colon cancer, colorectal cancer, craniopharyngioma, cystadenocarcinoma, dysproliferative changes (dysplasias and metaplasias), embryonal carcinoma, endometrial cancer, endotheliosarcoma, ependymoma, epithelial carcinoma, erythroleukemia, esophageal cancer, estrogen-receptor positive breast cancer, essential thrombocythemia, Ewing's tumor, fibrosarcoma, gastric carcinoma, germ cell testicular cancer, gestational trophobalstic disease, glioblastoma, head and neck cancer, heavy chain disease, hemangioblastoma, hepatoma, hepatocellular cancer, hormone insensitive prostate cancer, leiomyosarcoma, liposarcoma, lung cancer (including small cell lung cancer and non-small cell lung cancer), lymphangioendothelio-sarcoma, lymphangiosarcoma, lymphoblastic leukemia, lymphoma (lymphoma, including diffuse large B-cell lymphoma, follicular lymphoma, Hodgkin's lymphoma and non-Hodgkin's lymphoma), malignancies and hyperproliferative disorders of the bladder, breast, colon, lung, ovaries, pancreas, prostate, skin and uterus, lymphoid malignancies of T-cell or B-cell origin, leukemia, medullary carcinoma, medulloblastoma, melanoma, meningioma, mesothelioma, multiple myeloma, myelogenous leukemia, myeloma, myxosarcoma, neuroblastoma, oligodendroglioma, oral cancer, osteogenic sarcoma, ovarian cancer, pancreatic cancer, papillary adenocarcinomas, papillary carcinoma, peripheral T-cell lymphoma, pinealoma, polycythemia vera, prostate cancer (including hormone-insensitive (refractory) prostate cancer), rectal cancer, renal cell carcinoma, retinoblastoma, rhabdomyosarcoma, sarcoma, sebaceous gland carcinoma, seminoma, skin cancer, small cell lung carcinoma, solid tumors (carcinomas and sarcomas), stomach cancer, squamous cell carcinoma, synovioma, sweat gland carcinoma, testicular cancer (including germ cell testicular cancer), thyroid cancer, Waldenstrm's macroglobulinemia, testicular tumors, uterine cancer, Wilms' tumor and the like.

Abnormal activation of the Rho/ROCK pathway has been observed in various disorders (Wettschureck, N., Offermanns, S., Rho/Rho-kinase mediated signaling in physiology and pathophysiology. J. Mol. Med. 80, 2002, 629-638; Miller, B. K., Mack, H., Teusch, N., Rho kinase, a promising drug target for neurological discorders. Nat. Drug Discov. Rev. 4, 2005, 387-398; Hu, E, Lee, D., ROCK inhibitors as potential therapeutic agents for cardiovascular diseases. Curr. Opin. Investig. Drugs. 4, 2003, 1065-1075). As already mentioned, ROCKs phosphorylate the myosin binding subunit of myosin light chain (MLC) phosphatase (MLCP), resulting in increased myosin phosphorylation and actin-myosin contraction (Somlyo, A. P., Somlyo, A. V., Ca2+ sensitivity of smooth muscle and nonmuscle myosin II: modulated by G proteins, kinases, and myosin phosphatase. Physiol. Rev. 83, 2003, 1325-1358). Examples of disease states related with abnormal Rho/ROCK activity, in particular with vasospasm activity, include cardiovascular diseases such as hypertension (Satoh S., Kreutz R., Wilm C., Ganten D., Pfitzer G., Augmented agonist-induced Ca²⁺-sensitization of coronary artery contraction in genetically hypertensive rats. Evidence for altered signal transduction in the coronary smooth muscle cells. J. Clin. Invest. 94, 1994, 1397-1403; Mukai, Y., Shimokawa, H., Matoba, T., Kandabashi, T., Satoh, S., Hiroki, J., Kaibuchi, K., Takeshita, A., Involvement of Rho-kinase in hypertensive vascular disease: a novel therapeutic target in hypertension. FASEB J. 15, 2001, 1062-1064; Uehata, M., Ishizaki, T., Satoh, H., Ono, T., Kawahara, T., Morishita, T., Tamakawa, H., Yamagami, K., Inui, J., Maekawa, M., Narumiya, S., Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature 389, 1997, 990-994; Masumoto, A., Hirooka, Y., Shimokawa, H., Hironaga, K., Setoguchi, S., Takeshita, A., Possible involvement of Rhokinase in the pathogenesis of hypertension in humans. Hypertension 38, 2001, 1307-1310), chronic and congestive heart failure (Fuster, V., Badimon, L., Badimon, J J, Chesebro, J H, The pathogenesis of coronary artery disease and the acute coronary syndromes (2). N Engl J Med 326, 1992, 310-318; Shimokawa, H., Cellular and molecular mechanisms of coronary artery spasm: lessons from animal models. Jpn Circ J 64, 2000, 1-12; Shimokawa, H., Morishige, K., Miyata, K., Kandabashi, T., Eto, Y., Ikegaki, I., Asano, T., Kaibuchi, K., Takeshita, A., Longterm inhibition of Rho-kinase induces a regression of arteriosclerotic coronary lesions in a porcine model in vivo. Cardiovasc Res 51, 2001, 169-177; Utsunomiya, T., Satoh, S., Ikegaki, I., Toshima, Y., Asano, T., Shimokawa, H., Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina. Br J Pharmacol 134, 201, 1724-1730), cardiac hypertrophy (Hoshijima, M., Sah, V. P., Wang, Y., Chien, K. R., Brown, J. H., The low molecular weight GTPase Rho regulates myofibril formation and organization in neonatal rat ventricular myocytes. Involvement of Rho kinase. J Biol Chem 273, 1998, 7725-77230; Sah, V. P., Hoshijima, M., Chien, K. R., Brown, J. H., Rho is required for Galphaq and alpha1-adrenergic receptor signal-637 ing in cardiomyocytes. Dissociation of Ras and Rho pathways. J Biol Chem 271, 1996, 31185-1190; Kuwahara, K., Saito, Y., Nakagawa, O., Kishimoto, I., Harada, M., Ogawa, E., Miyamoto, Y., Hamanaka, I., Kajiyama, N., Takahashi, N., Izumi, T., Kawakami, R., Tamura, N., Ogawa, Y., Nakao, K., The effects of the selective ROCK inhibitor, Y27632, on ET-1-induced hypertrophic response in neonatal rat cardiacmyocytes-possible involvement of Rho/ROCK pathway in cardiac muscle cell hypertrophy. FEBS Lett 452, 1999, 314-318), chronic renal failure (Sharpe, C. C., Hendry, B., M. Signaling: focus on Rho in renal disease. J. Am. Soc. Nephrol. 14, 2003, 261-264), cerebral vasospasm after subarachnoid bleeding (Shibuya, M., Suzuki, Y., Sugita, K., Saito, I., Sasaki, T., Takakura, K., Okamoto, S., Kikuchi, H., Takemae, T., Hidaka, H., Dose escalation trial of a novel calcium antagonist, AT877, in patients 636 with aneurysmal subarachnoid haemorrhage. Acta Neurochir (Wien) 107, 1990, 11-15; Shibuya, M., Suzuki, Y., Sugita, K., Saito, I., Sasaki, T., Takakura, K., Nagata, I., Kikuchi, H., Takemae, T., Hidaka, H., et. al, Effect of AT877 on cerebral vasospasm after aneurysmal subarachnoid hemorrhage. Results of a prospective placebo-controlled double-blind trial. J Neurosurg 76, 1992, 571-577; Sato, M., Tani, E., Fujikawa, H., Kaibuchi, K., Involvement of Rho-kinase-mediated phosphorylation of myosin light chain in enhancement of cerebral vasospasm. Circ Res 87, 2000, 195-200; Miyagi, Y., Carpenter, R. C., Meguro, T., Parent, A. D., Zhang, J. H., Upregulation of rho A and rho kinase messenger RNAs in the basilar artery of a rat model of subarachnoid hemorrhage. J Neurosurg 93, 2000, 471-476; Tachibana, E., Harada, T., Shibuya, M. Saito, K., Takayasu, M., Suzuki, Y., Yoshida, J., Intra-arterial infusion of fasudil hydrochloride for treating vasospasm following subarachnoid haemorrhage. Acta Neurochir (Wien) 141, 1999, 13-19), pulmonary hypertension (Sylvester, J. T., Am. J. Physiol. Lung Cell. Mol. Physiol. 287, 2004, L624-L630) and ocular hypertension (Honjo, M., Inatani, M., Kido, N., Sawamura, T., Yue, B. Y., Honda, Y., Tanihara, H., Effects of protein kinase inhibitor, HA1077, on intraocular pressure and outflow facility in rabbit eyes. Arch Ophthalmol 119, 2001, 1171-1178; Rao, P. V., Deng, P. F., Kumar, J. Epstein, D. L., Modulation of aqueous humor outflow facility by the Rho kinase-specific inhibitor Y-27632. Invest Ophthalmol Vis Sci 42, 2001, 1029-1037). Further diseases related to abnormal Rho/ROCK activity are cancer (Aznar, S., Fernandez-Valeron, P., Espina, C., Lacal, J. C., Rho GTPases: potential candidates for anticancer therapy. Cancer Lett. 206, 2004, 181-191; Yin, L. et al., Fasudil inhibits vascular endothelial growth factor-induced angiogenesis in vitro and in vivo. Mol Cancer Ther 5, 2007, 1517-25; Itoh, K., Yoshioka, K., Akedo, H., Uehata, M., Ishizaki, T., Narumiya, S., An essential part for Rho-associated kinase in the transcellular invasion of tumor cells. Nat Med 5, 1999, 221-225; Genda, T. Sakamoto, M., Ichida, T., Asakura, H., Kojiro, M., Narumiya, S., Hirohashi, S., Cell motility mediated by rho and Rho-associated protein kinase plays a critical role inintrahepatic metastasis of human hepatocellular carcinoma. Hepatology 30, 1999, 1027-1036; Somlyo, A. V., Bradshaw, D., Ramos, S., Murphy, C., Myers, C. E., Somlyo, A. P., Rho-kinase inhibitor retards migration and in vivo dissemination of human prostate cancer cells. Biochem Biophys Res Commun 269, 2000, 652-659), asthma (Roberts, J. A., Raeburn, D., Rodger, I. W., Thomson, N. C., Comparison of in vivo airway responsiveness and in vitro smooth muscle sensitivity to methacholine in man. Thorax 39; 1984, 837-843; Chiba, Y., Misawa, M., Characteristics of muscarinic cholinoceptors in airways of antigen-induced airway hyperresponsive rats. Comp Biochem Physiol C Pharmacol Toxicol Endocrinol 111, 1995, 351-357; Chiba, Y., Takada, Y., Miyamoto, S., MitsuiSaito, M., Karaki, H., Misawa, M., Augmented acetylcholine-induced, Rho mediated Ca²⁺ sensitization of bronchial smooth muscle contraction in antigen-induced airway hyperresponsive rats. Br J Pharmacol 127, 1999, 597-600; Chiba, Y., Sakai, H. Misawa, M., Augmented acetylcholine-induced translocation of RhoA in bronchial smooth muscle from antigen-induced airway hyperresponsive rats. Br J Pharmacol 133, 2001, 886-890; Iizuka, K., Shimizu, Y., Tsukagoshi, H., Yoshii, A., Harada, T. Dobashi, K., Murozono, T., Nakazawa, T., Mori, M., Evaluation of Y-27632, a rho-kinase inhibitor, as a bronchodilator in guinea pigs. Eur J Pharmacol 406, 2000, 273-279), male erectile dysfunctions (Andersson, K. E., Hedlund, P., New directions for erectile dysfunction therapies. Int. J. Impot. Res. 14 (Suppl. 1), 2002, S82S92; Chitaley, K., Wingard, C. J., Clinton Webb, R., Branam, H., Stopper, V. S., Lewis, R. W., Mills, T. M., Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxideindependent pathway. Nat Med 7, 2001, 119-122; Mills, T. M., Chitaley, K., Wingard, C. J., Lewis, R. W., Webb, R. C., Effect of Rho-kinase inhibition on vasoconstriction in the penile circulation. J Appl Physiol 91, 2001, 1269-1273), female sexual dysfunction, over-active bladder syndrome (Peters, S. L. et al., Rho kinase: a target for treating urinary bladder dysfunction. Trends Pharmacol Sci. 27, 2006, 492-7) and preterm labor (Niiro, N., Nishimura, J., Sakihara, C., Nakano, H., Kanaide, H., Up-regulation of rho A and rho-kinase mRNAs in the rat myometrium during pregnancy. Biochem Biophys Res Commun 230, 1997, 356-359; Tahara, M., Morishige, K., Sawada, K., Ikebuchi, Y., Kawagishi, R., Tasaka, K., Murata, Y., RhoA/Rho-kinase cascade is involved in oxytocin-induced rat uterine contraction. Endocrinology 143, 2002, 920-929; Kupittayanant, S., Burdyga, T., Wray, S., The effects of inhibiting Rho-associated kinase with Y-27632 on force and intracellular calcium in human myometrium. Pflugers Arch. 443, 2001, 112-114).

Inhibitors of ROCKs have been suggested for use in the treatments of a variety of diseases. They include cardiovascular diseases such as hypertension (Satoh S., Kreutz R., Wilm C., Ganten D., Pfitzer G., Augmented agonist-induced Ca²⁺-sensitization of coronary artery contraction in genetically hypertensive rats. Evidence for altered signal transduction in the coronary smooth muscle cells. J. Clin. Invest. 94, 1994, 1397-1403; Mukai, Y., Shimokawa, H., Matoba, T., Kandabashi, T., Satoh, S., Hiroki, J., Kaibuchi, K., Takeshita, A., Involvement of Rho-kinase in hypertensive vascular disease: a novel therapeutic target in hypertension. FASEB J. 15, 2001, 1062-1064; Uehata, M., Ishizaki, T., Satoh, H., Ono, T., Kawahara, T., Morishita, T., Tamakawa, H., Yamagami, K., Inui, J., Maekawa, M., Narumiya, S., Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature 389, 1997, 990-994; and Masumoto, A., Hirooka, Y., Shimokawa, H., Hironaga, K., Setoguchi, S., Takeshita, A., Possible involvement of Rhokinase in the pathogenesis of hypertension in humans. Hypertension 38, 2001, 1307-1310), chronic and congestive heart failure (Fuster, V., Badimon, L., Badimon, J J, Chesebro, J H, The pathogenesis of coronary artery disease and the acute coronary syndromes (2). N Engl J Med 326, 1992, 310-318; Shimokawa, H., Cellular and molecular mechanisms of coronary artery spasm: lessons from animal models. Jpn Circ J 64, 2000, 1-12; Shimokawa, H., Morishige, K., Miyata, K., Kandabashi, T., Eto, Y., Ikegaki, I., Asano, T., Kaibuchi, K., Takeshita, A., Longterm inhibition of Rho-kinase induces a regression of arteriosclerotic coronary lesions in a porcine model in vivo. Cardiovasc Res 51, 2001, 169-177; Utsunomiya, T., Satoh, S., Ikegaki, I., Toshima, Y., Asano, T., Shimokawa, H., Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina. Br J Pharmacol 134, 201, 1724-1730), cardiac hypertrophy), and cardiac hypertrophy (Hoshijima, M., Sah, V. P., Wang, Y., Chien, K. R., Brown, J. H., The low molecular weight GTPase Rho regulates myofibril formation and organization in neonatal rat ventricular myocytes. Involvement of Rho kinase. J Biol Chem 273, 1998, 7725-77230; Sah, V. P., Hoshijima, M., Chien, K. R., Brown, J. H., Rho is required for Galphaq and alpha1-adrenergic receptor signal-637 ing in cardiomyocytes. Dissociation of Ras and Rho pathways. J Biol Chem 271, 1996, 31185-1190; Kuwahara, K., Saito, Y., Nakagawa, O., Kishimoto, I., Harada, M., Ogawa, E., Miyamoto, Y., Hamanaka, I., Kajiyama, N., Takahashi, N., Izumi, T., Kawakami, R., Tamura, N., Ogawa, Y., Nakao, K., The effects of the selective ROCK inhibitor, Y27632, on ET-1-induced hypertrophic response in neonatal rat cardiacmyocytes-possible involvement of Rho/ROCK pathway in cardiac muscle cell hypertrophy. FEBS Lett 452, 1999, 314-318), chronic renal failure), chronic renal failure (Sharpe, C. C., Hendry, B., M. Signaling: focus on Rho in renal disease. J. Am. Soc. Nephrol. 14, 2003, 261-264), furthermore cerebral vasospasm after subarachnoid bleeding (Shibuya, M., Suzuki, Y., Sugita, K., Saito, I., Sasaki, T., Takakura, K., Okamoto, S., Kikuchi, H., Takemae, T., Hidaka, H., Dose escalation trial of a novel calcium antagonist, AT877, in patients 636 with aneurysmal subarachnoid haemorrhage. (Acta Neurochir (Wien) 107, 1990, 11-15; Shibuya, M., Suzuki, Y., Sugita, K., Saito, I., Sasaki, T., Takakura, K., Nagata, I., Kikuchi, H., Takemae, T., Hidaka, H., et. al, Effect of AT877 on cerebral vasospasm after aneurysmal subarachnoid hemorrhage. Results of a prospective placebo-controlled double-blind trial. J Neurosurg 76, 1992, 571-577; Sato, M., Tani, E., Fujikawa, H., Kaibuchi, K., Involvement of Rho-kinase-mediated phosphorylation of myosin light chain in enhancement of cerebral vasospasm. Circ Res 87, 2000, 195-200; Miyagi, Y., Carpenter, R. C., Meguro, T., Parent, A. D., Zhang, J. H., Upregulation of rho A and rho kinase messenger RNAs in the basilar artery of a rat model of subarachnoid hemorrhage. J Neurosurg 93, 2000, 471-476; Tachibana, E., Harada, T., Shibuya, M. Saito, K., Takayasu, M., Suzuki, Y., Yoshida, J., Intra-arterial infusion of fasudil hydrochloride for treating vasospasm following subarachnoid haemorrhage. Acta Neurochir (Wien) 141, 1999, 13-19), pulmonary hypertension (Sylvester, J. T., Am. J. Physiol. Lung Cell. Mol. Physiol. 287, 2004, L624-L630) and ocular hypertension (Honjo, M., Inatani, M., Kido, N., Sawamura, T., Yue, B. Y., Honda, Y., Tanihara, H., Effects of protein kinase inhibitor, HA1077, on intraocular pressure and outflow facility in rabbit eyes. Arch Ophthalmol 119, 2001, 1171-1178; Rao, P. V., Deng, P. F., Kumar, J. Epstein, D. L., Modulation of aqueous humor outflow facility by the Rho kinase-specific inhibitor Y-27632. Invest Ophthalmol Vis Sci 42, 2001, 1029-1037). In addition, because of their muscle relaxing properties, they are also suitable for asthma (Roberts, J. A., Raeburn, D., Rodger, I. W., Thomson, N. C., Comparison of in vivo airway responsiveness and in vitro smooth muscle sensitivity to methacholine in man. Thorax 39; 1984, 837-843; Chiba, Y., Misawa, M., Characteristics of muscarinic cholinoceptors in airways of antigen-induced airway hyperresponsive rats. Comp Biochem Physiol C Pharmacol Toxicol Endocrinol 111, 1995, 351-357; Chiba, Y., Takada, Y., Miyamoto, S., MitsuiSaito, M., Karaki, H., Misawa, M., Augmented acetylcholine-induced, Rho mediated Ca²⁺ sensitization of bronchial smooth muscle contraction in antigen-induced airway hyperresponsive rats. Br J Pharmacol 127, 1999, 597-600; Chiba, Y., Sakai, H. Misawa, M., Augmented acetylcholine-induced translocation of RhoA in bronchial smooth muscle from antigen-induced airway hyperresponsive rats. Br J Pharmacol 133, 2001, 886-890; fizuka, K., Shimizu, Y., Tsukagoshi, H., Yoshii, A., Harada, T. Dobashi, K., Murozono, T., Nakazawa, T., Mori, M., Evaluation of Y-27632, a rho-kinase inhibitor, as a bronchodilator in guinea pigs. Eur J Pharmacol 406, 2000, 273-279), male erectile dysfunctions (Andersson, K. E., Hedlund, P., New directions for erectile dysfunction therapies. Int. J. Impot. Res. 14 (Suppl. 1), 2002, S82-S92; Chitaley, K., Wingard, C. J., Clinton Webb, R., Branam, H., Stopper, V. S., Lewis, R. W., Mills, T. M., Antagonism of Rho-kinase stimulates rat penile erection via a nitric oxideindependent pathway. Nat Med 7, 2001, 119-122; Mills, T. M., Chitaley, K., Wingard, C. J., Lewis, R. W., Webb, R. C., Effect of Rho-kinase inhibition on vasoconstriction in the penile circulation. J Appl Physiol 91, 2001, 1269-1273), female sexual dysfunction and over-active bladder syndrome (Peters, S. L. et al., Rho kinase: a target for treating urinary bladder dysfunction. Trends Pharmacol Sci. 27, 2006, 492-7) and preterm labor (Niiro, N., Nishimura, J., Sakihara, C., Nakano, H., Kanaide, H., Up-regulation of rho A and rho-kinase mRNAs in the rat myometrium during pregnancy. Biochem Biophys Res Commun 230, 1997, 356-359; Tahara, M., Morishige, K., Sawada, K., Ikebuchi, Y., Kawagishi, R., Tasaka, K., Murata, Y., RhoA/Rho-kinase cascade is involved in oxytocin-induced rat uterine contraction. Endocrinology 143, 2002, 920-929; Kupittayanant, S., Burdyga, T., Wray, S., The effects of inhibiting Rho-associated kinase with Y-27632 on force and intracellular calcium in human myometrium. Pflugers Arch. 443, 2001, 112-114). Several recent studies have reported the beneficial effects of ROCK inhibitors in ischemia-reperfusion and myocardial infarction. In these studies, the ROCK inhibitors Y-27632 and fasudil were shown to decrease ischemia-reperfusion injury, myocardial infarct size, and myocardial fibrosis in response to experimental myocardial infarction (MI) and in a rat model of chronic hypertension induced congestive heart failure (see above (Fuster, V., Badimon, L., Badimon, J J, Chesebro, J H, The pathogenesis of coronary artery disease and the acute coronary syndromes (2). N Engl J Med 326, 1992, 310-318; Shimokawa, H., Cellular and molecular mechanisms of coronary artery spasm: lessons from animal models. Jpn Circ J 64, 2000, 1-12; Shimokawa, H., Morishige, K., Miyata, K., Kandabashi, T., Eto, Y., Ikegaki, I., Asano, T., Kaibuchi, K., Takeshita, A., Longterm inhibition of Rho-kinase induces a regression of arteriosclerotic coronary lesions in a porcine model in vivo. Cardiovasc Res 51, 2001, 169-177; Utsunomiya, T., Satoh, S., Ikegaki, I., Toshima, Y., Asano, T., Shimokawa, H., Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina. Br J Pharmacol 134, 201, 1724-1730), cardiac hypertrophy) and Masumoto, A., Mohri, M., Shimokaw, a H., Urakami, L., Usui, M., Takeshita, A., Suppression of coronary artery spasm by the rho-kinase inhibitor fasudil in patients with vasospastic angina. Circulation 105, 2002, 1545-1547; Shimokawa, H., linuma, H., Kishida, H., et al., Antianginal effect of fasudil, a Rho-kinase inhibitor, in patients with stable effort angina: a multicenter study (abstract). Circulation 104[Suppl II], 2001, 11691; Morishige K, Shimokawa H, Eto Y, Kandabashi T, Miyata K, Matsumoto Y, Hoshijima M, Kaibuchi K, Takeshita A, Adenovirus-mediated transfer of dominant-negative rho-kinase induces a regression of coronary arteriosclerosis in pigs in vivo. Arterioscler Thromb Vasc Biol 21, 2001, 548-554; Kandabashi T, Shimokawa H, Mukai Y, Matoba T, Kunihiro I, Morikawa K, Ito M, Takahashi S, Kaibuchi K, Takeshita A, Involvement of rho-kinase in agonists-induced contractions of arteriosclerotic human arteries. Arterioscler Thromb Vasc Biol 22, 2002, 243-248; Liu M W, Roubin G S, King S B 3^(rd), Restenosis after coronary angioplasty. Potential biologic determinants and role of intimal hyperplasia. Circulation 79, 1989, 1374-1387; Shibata R, Kai H, Seki Y, Kato S, Morimatsu M, Kaibuchi K, Imaizumi T, Role of Rho-associated kinase in neointima formation after vascular injury. Circulation 103, 2001, 284-289).

Additionally, ROCKs can interact with other signalling pathways resulting in inhibition of phosphoinositide-3 kinase (PI-3K), endothelial nitric oxide synthase (eNOS) pathways, and activation of plasminogen activator inhibitor-1 (PAI-1) which may contribute to endothelial dysfunction like restenosis and atherosclerosis. Thus ROCK inhibitors have been suggested for the treatment of restenosis and atherosclerosis (see above (Morishige K, Shimokawa H, Eto Y, Kandabashi T, Miyata K, Matsumoto Y, Hoshijima M, Kaibuchi K, Takeshita A, Adenovirus-mediated transfer of dominant-negative rho-kinase induces a regression of coronary arteriosclerosis in pigs in vivo. Arterioscler Thromb Vasc Biol 21, 2001, 548-554; Kandabashi T, Shimokawa H, Mukai Y, Matoba T, Kunihiro I, Morikawa K, Ito M, Takahashi S, Kaibuchi K, Takeshita A, Involvement of rho-kinase in agonists-induced contractions of arteriosclerotic human arteries. Arterioscler Thromb Vasc Biol 22, 2002, 243-248; Liu M W, Roubin G S, King S B 3^(rd), Restenosis after coronary angioplasty. Potential biologic determinants and role of intimal hyperplasia. Circulation 79, 1989, 1374-1387; Shibata R, Kai H, Seki Y, Kato S, Morimatsu M, Kaibuchi K, Imaizumi T, Role of Rho-associated kinase in neointima formation after vascular injury. Circulation 103, 2001, 284-289) and Iwasaki, H. et al., High glucose induces plasminogen activator inhibitor-1 expression through Rho/Rho-kinase-mediated NF-kappaB activation in bovine aortic endothelial cells. Atherosclerosis, 2007, Jan. 31).

Vascular intimal thickening in vein grafts after surgery is the major cause of late graft failure. In a study with the ROCK inhibitor fasudil, the intimal thickening and vascular smooth muscle cell (VSMC) proliferation was significantly suppressed, whereas VSMC apoptosis was enhanced in the weeks following the procedure, suggesting that ROCK inhibitors can be used as a therapeutic agent for the prevention of graft (Morishige K, Shimokawa H, Eto Y, Kandabashi T, Miyata K, Matsumoto Y, Hoshijima M, Kaibuchi K, Takeshita A, Adenovirus-mediated transfer of dominant-negative rho-kinase induces a regression of coronary arteriosclerosis in pigs in vivo. Arterioscler Thromb Vasc Biol 21, 2001, 548-554; Kandabashi T, Shimokawa H, Mukai Y, Matoba T, Kunihiro I, Morikawa K, Ito M, Takahashi S, Kaibuchi K, Takeshita A, Involvement of rho-kinase in agonists-induced contractions of arteriosclerotic human arteries. Arterioscler Thromb Vasc Biol 22, 2002, 243-248; Liu M W, Roubin G S, King S B 3^(rd), Restenosis after coronary angioplasty. Potential biologic determinants and role of intimal hyperplasia. Circulation 79, 1989, 1374-1387; Shibata R, Kai H, Seki Y, Kato S, Morimatsu M, Kaibuchi K, Imaizumi T, Role of Rho-associated kinase in neointima formation after vascular injury. Circulation 103, 2001, 284-289).

Injury to the adult vertebrate brain and spinal cord activates ROCKs, thereby causing neurodegeneration and inhibition of neuroregeneration like neurite growth and sprouting (Bito, H., Furuyashiki, T., Ishihara, H., Shibasaki, Y., Ohashi, K., Mizuno, K., Maekawa, M., Ishizaki, T., Narumiya, S., A critical role for a Rho-associated kinase, p160ROCK, in determining axon outgrowth in mammalian CNS neurons. Neuron 26, 2000, 431-441). Inhibition of ROCKs results in induction of new axonal growth, axonal rewiring across lesions within the CNS, accelerated regeneration and enhanced functional recovery after acute neuronal injury in mammals (spinal-cord injury, traumatic brain injury) (see above (Peters, S. L. et al., Rho kinase: a target for treating urinary bladder dysfunction. Trends Pharmacol Sci. 27, 2006, 492-7) and Hara, M. et al., Protein kinase inhibition by fasudil hydrochloride promotes neurological recovery after spinal cord injury in rats. J. Neurosurg. Spine 93, 94-101; Fournier, A. E., Takizawa, B. T. & Strittmatter, S. M., ROCK inhibition enhances axonal regeneration in the injured CNS. J. Neurosci. 23, 2003, 1416-1423; Sung, J. K. et al., A possible role of RhoA/Rho-kinase in experimental spinal cord injury in rat. Brain Res. 959, 2003, 29-38; Tanaka, H. et al., Cytoplasmic p21(Cip1/WAF1) enhances axonal regeneration and functional recovery after spinal cord injury in rats. Neuroscience 127, 2004, 155-164). ROCK inhibitors are therefore likely to be useful for regenerative (recovery) treatment of CNS disorders such as spinal cord injury, acute neuronal injury (stroke, traumatic brain injury) (Okamura N et al., Vasodilator effects of fasudil, a Rho-kinase inhibitor, on retinal arterioles in stroke-prone spontaneously hypertensive rats. J Ocul Pharmacol Ther. 23, 2007, 207-12; Yagita Y et al., Rho-kinase activation in endothelial cells contributes to expansion of infarction after focal cerebral ischemia. J Neurosci Res. 85, 2007, 2460-9), Parkinson's disease, Alzheimer disease (Pedrini S et al., Modulation of statin-activated shedding of Alzheimer APP ectodomain by ROCK. PLoS Med. 2, 2005, 18; Burton A., NSAIDS and Alzheimer's disease: it's only Rock and Rho. Lancet Neurol. 3(1), 2004, 6) and other neurodegenerative disorders. Other neurodegenetarive disorders for which ROCK inhibitors are expected to be useful are Huntington's disease (Shao J, Welch W J, Diprospero N A, Diamond M I. Phosphorylation of profilin by ROCK1 regulates polyglutamine aggregation. Mol Cell Biol. 2008 September; 28(17):5196-208; Shao J, Welch W J, Diamond M I. ROCK and PRK-2 mediate the inhibitory effect of Y-27632 on polyglutamine aggregation. FEBS Lett. 2008 May 28; 582(12):1637-42), spinal muscular atrophy (Bowerman M, Shafey D, Kothary R., Smn depletion alters profilin II expression and leads to upregulation of the RhoA/ROCK pathway and defects in neuronal integrity. J Mol Neurosci. 2007; 32(2):120-31) and amyotrophic lateral sclerosis. Inhibition of the Rho/ROCK pathway has also proved to be efficacious in other animal models of neurodegeneration like stroke (Okamura N et al., Vasodilator effects of fasudil, a Rho-kinase inhibitor, on retinal arterioles in stroke-prone spontaneously hypertensive rats. J Ocul Pharmacol Ther. 23, 2007, 207-12; Yagita Y et al., Rho-kinase activation in endothelial cells contributes to expansion of infarction after focal cerebral ischemia. J Neurosci Res. 85, 2007, 2460-9) and in inflammatory and demyelinating diseases like multiple sclerosis (Sun X et al., The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 180, 2006, 126-34), acute and chronic pain (Inoue, M. et al., Initiation of neuropathic pain requires lysophosphatidic acid receptor signaling. Nature Med. 10, 2004, 712-718; Ramer, L. M., Borisoff, J. F. & Ramer, M. S., Rho-kinase inhibition enhances axonal plasticity and attenuates cold hyperalgesia after dorsal rhizotomy. J Neurosci. 24, 2004, 10796-10805; Tatsumi, S. et al., Involvement of Rho-kinase in inflammatory and neuropathic pain through phosphorylation of myristoylated alanine-rich C-kinase substrate (MARCKS). Neuroscience 131, 2005, 491-498).

ROCK inhibitors have been shown to possess anti-inflammatory properties by decreased cytokine release, e.g. TNFα. Thus they can be used as treatment for neuroinflammatory diseases such as stroke, multiple sclerosis, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis and inflammatory pain, as well as other inflammatory diseases such as rheumatoid arthritis, osteoarthritis, osteoporosis, asthma, irritable bowel syndrome, or inflammatory bowel disease (Segain J. P., Rho kinase blockade prevents inflammation via nuclear factor kappa B inhibition: evidence in Crohn's disease and experimental colitis. Gastroenterology. 124(5), 2003, 1180-7). In addition, recent reports have demonstrated that inhibition of ROCK results in disruption of inflammatory cell chemotaxis as well as inhibition of smooth muscle contraction in models of pulmonary inflammation associated with asthma. Therefore, the inhibitors of the Rho/ROCK pathway should be useful for the treatment of asthma (see above (Sun X et al., The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 180, 2006, 126-34) and Kawaguchi A, Ohmori M, Harada K, Tsuruoka S, Sugimoto K, Fujimura A., The effect of a Rho kinase inhibitor Y-27632 on superoxide production, aggregation and adhesion inhuman polymorphonuclear leukocytes. Eur J Pharmacol 403, 2000, 203-208; Lou Z, Billadeau D D, Savoy D N, Schoon R A, Leibson P. J., A role for a RhoA/ROCK/LIM-kinase pathway in the regulation of cytotoxic lymphocytes. J Immunol 167, 2001, 5749-5757; Vicente-Manzanares M, Cabrero J R, Rey M, Perez-Martinez M, Ursa A, Itoh K, Sanchez-Madrid F., A role for the Rho-p160 Rho coiled-coil kinase axis in the chemokine stromal cell-derived factor-1alpha-induced lymphocyte actomyosinand microtubular organization and chemotaxis. J Immunol 168, 2002, 400-410; Thorlacius K et al., Protective effect of fasudil, a Rho-kinase inhibitor, on chemokine expression, leukocyte recruitment, and hepatocellular apoptosis in septic liver injury. J Leukoc Biol. 79, 2006, 923-31).

Since ROCK inhibitors reduce cell proliferation and cell migration, they could be useful in treating cancer and tumor metastasis (Aznar, S., Fernandez-Valeron, P., Espina, C., Lacal, J. C., Rho GTPases: potential candidates for anticancer therapy. Cancer Lett. 206, 2004, 181-191; Yin, L. et al., Fasudil inhibits vascular endothelial growth factor-induced angiogenesis in vitro and in vivo. Mol Cancer Ther 5, 2007, 1517-25. Itoh, K., Yoshioka, K., Akedo, H., Uehata, M., Ishizaki, T., Narumiya, S., An essential part for Rho-associated kinase in the transcellular invasion of tumor cells. Nat Med 5, 1999, 221-225; Genda, T. Sakamoto, M., Ichida, T., Asakura, H., Kojiro, M., Narumiya, S., Hirohashi, S., Cell motility mediated by rho and Rho-associated protein kinase plays a critical role inintrahepatic metastasis of human hepatocellular carcinoma. Hepatology 30, 1999, 1027-1036; Somlyo, A. V., Bradshaw, D., Ramos, S., Murphy, C., Myers, C. E., Somlyo, A. P., Rho-kinase inhibitor retards migration and in vivo dissemination of human prostate cancer cells. Biochem Biophys Res Commun 269, 2000, 652-659). ROCK inhibitors can also be beneficial in diseases with impaired blood brain barrier function, e.g. HIV-1 encephalitis (Persidski Y et al., Rho-mediated regulation of tight junctions during monocyte migration across the blood-brain barrier in HIV-1 encephalitis (HIVE). Blood. 107, 2006, 4770-4780) and Alzheimer's disease (Man S-M et al., Peripheral T cells overexpress MIP-1a to enhance its transendothelial migration in Alzheimer's disease. Neurobiol. Of Aging 28, 2007, 485-496).

Furthermore, there is evidence suggesting that ROCK inhibitors suppress cytoskeletal rearrangement upon virus invasion, thus they also have potential therapeutic value in anti-viral and anti-bacterial applications (Favoreel H W, Cytoskeletal rearrangements and cell extensions induced by the US3 kinase of an alphaherpesvirus are associated with enhanced spread. Proc Natl Acad Sci USA. 102(25), 2006, 8990-5).

ROCKs have been reported to interfere with insulin signalling through serine phosphorylation of insulin receptor substrate-1 (IRS-1), in cultured VSMC. Activation of RhoA/ROCK was observed in skeletal muscles and aortic tissues of Zucker obese rats. Inhibition of ROCK, by fasudil for 4 weeks, reduced blood pressure, corrected glucose and lipid metabolism, improved insulin signalling and endothelial dysfunction. In another experiment administration of high dose fasudil completely suppressed the development of diabetes, obesity, and dyslipidemia and increased serum adiponectin levels in OLETF rats. ROCK inhibitors may therefore be useful for the treatment of insulin resistance and diabetes (Nakamura Y et al., Marked increase of insulin gene transcription by suppression of the Rho/Rho-kinase pathway. Biochem Biophys Res Commun 350(1), 2006, 68-73; Kikuchi Y et al., A Rho-kinase inhibitor, fasudil, prevents development of diabetes and nephropathy in insulin-resistant diabetic rats. J Endocrinol. 192(3), 2007, 595-603; Goyo A et al., The Rho-kinase inhibitor, fasudil, attenuates diabetic nephropathy in streptozotocin-induced diabetic rats. Eur J Pharmacol. 568(1-3), 2007, 242-7).

The ROCK inhibitor Fasudil increased cerebral blood flow and was neuroprotective under CNS ischemic conditions. ROCK inhibitors are expected to be useful for the treatment of ischemic CNS disorders and may therefore improve functional outcome in patients suffering from stroke, vascular or AD type dementia (Okamura N et al., Vasodilator effects of fasudil, a Rho-kinase inhibitor, on retinal arterioles in stroke-prone spontaneously hypertensive rats. J Ocul Pharmacol Ther. 23, 2007, 207-12; Yagita Y et al., Rho-kinase activation in endothelial cells contributes to expansion of infarction after focal cerebral ischemia. J Neurosci Res. 85, 2007, 2460-9).

Due to the efficacy of Y-27632 and fasudil in animal models of epileptogenesis, ROCK inhibitors have been suggested for the use in the treatments of epilepsy and seizure disorders (Inan S Y, Büyükafsar K. Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. Br. J. Pharmacol. advance online publication, 9 Jun. 2008; doi:10.1038/bjp.2008.225)

ROCK inhibitors are also expected to be useful for the treatment of glaucoma (Honjo, M., Inatani, M., Kido, N., Sawamura, T., Yue, B. Y., Honda, Y., Tanihara, H., Effects of protein kinase inhibitor, HA1077, on intraocular pressure and outflow facility in rabbit eyes. Arch Ophthalmol 119, 2001, 1171-1178; Rao, P. V., Deng, P. F., Kumar, J. Epstein, D. L., Modulation of aqueous humor outflow facility by the Rho kinase-specific inhibitor Y-27632. Invest Ophthalmol Vis Sci 42, 2001, 1029-1037), psoriasis, retinopathy and benign prostatic hypertrophy.

Furthermore, there is evidence suggesting that ROCK inhibitors suppress cytoskeletal rearrangement upon virus invasion, thus they also have potential therapeutic value in anti-viral and anti-bacterial applications.

As ROCKs have been implicated in neuronal morphogenesis, connectivity, and plasticity in general, they are expected to be useful for the treatment of psychiatric disorders, e.g. depression, schizophrenia, obsessive compulsive disorder and bipolar disorders.

ROCK inhibitors have been described in e.g. WO 2007/026920, WO 2005/074643, and WO 2004/016597. However, their affinity and selectivity or their pharmacological profile is not yet satisfactory.

SCHEMES AND EXPERIMENTALS

The following abbreviations have the meanings indicated. ADDP means 1,1′-(azodicarbonyl)dipiperidine; AD-mix-β means a mixture of (DHQD)₂PHAL, K₃Fe(CN)₆, K₂CO₃, and K₂SO₄; 9-BBN means 9-borabicyclo(3.3.1)nonane; Boc means tert-butoxycarbonyl; (DHQD)₂PHAL means hydroquinidine 1,4-phthalazinediyl diethyl ether; DBU means 1,8-diazabicyclo[5.4.0]undec-7-ene; DIBAL means diisobutylaluminum hydride; DIEA means diisopropylethylamine; DMAP means N,N-dimethylaminopyridine; DMF means N,N-dimethylformamide; dmpe means 1,2-bis(dimethylphosphino)ethane; DMSO means dimethylsulfoxide; dppb means 1,4-bis(diphenylphosphino)-butane; dppe means 1,2-bis(diphenylphosphino)ethane; dppf means 1,1′-bis(diphenylphosphino)ferrocene; dppm means 1,1-bis(diphenylphosphino)methane; EDACHC1 means 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride; Fmoc means fluorenylmethoxycarbonyl; HATU means O-(7-azabenzotriazol-1-yl)-N,N′N′N′-tetramethyluronium hexafluorophosphate; HMPA means hexamethylphosphoramide; IPA means isopropyl alcohol; MP-BH₃ means macroporous triethylammonium methylpolystyrene cyanoborohydride; TEA means triethylamine; TFA means trifluoroacetic acid; tetrahydrofuran means tetrahydrofuran; NCS means N-chlorosuccinimide; NMM means N-methylmorpholine; NMP means N-methylpyrrolidine; PPh₃ means triphenylphosphine.

The following schemes are presented to provide what is believed to be the most useful and readily understood description of procedures and conceptual aspects of this invention. Compounds of this invention may be made by synthetic chemical processes, examples of which are shown herein. It is meant to be understood that the order of the steps in the processes may be varied, that reagents, solvents and reaction conditions may be substituted for those specifically mentioned, and that vulnerable moieties may be protected and deprotected, as necessary.

SCHEMES

As shown in Scheme 1, compounds of formula (1), wherein X¹, X², and X³ are as described herein, can be reacted with methyl 4-isocyanatobenzoate to provide compounds of formula (2). The reaction is typically performed in a solvent such as but not limited to tetrahydrofuran. The methyl 4-isocyanatobenzoate is typically added at low temperature followed by stirring at room temperature. Compounds of formula (3) can be prepared by reacting compounds of formula (2) with aqueous lithium hydroxide. The reaction is typically performed in a solvent such as but not limited to tetrahydrofuran, methanol, or mixtures thereof. Compounds of formula (3) can be reacted with amine of formula (3A), wherein R⁵ is hydrogen or is as described herein, using coupling conditions known to those skilled in the art and readily available in the literature to provide compounds of formula (4), which are representative of the compounds of this invention.

As shown in Scheme 2, compounds of formula (1), wherein X¹, X², and X³ are as described herein, can be reacted with 4-nitrophenylisocyanate to provide compounds of formula (5). The reaction is typically performed in a solvent such as but not limited to tetrahydrofuran. Compounds of formula (5) can be treated with a hydrogen balloon in the presence of 10% Pd on carbon to provide compounds of formula (6). The reaction is typically performed at ambient temperature in a solvent such as but not limited to dimethylformamide. Compounds of formula (6) can be reacted with acid of formula (6A), wherein R⁵ is as described herein, using coupling conditions known to those skilled in the art and readily available in the literature to provide compounds of formula (7), which are representative of the compounds of this invention.

As shown in Scheme 3, compounds of formula (1), wherein X¹, X², and X³ are as described herein, can be reacted with 4-bromophenyl isocyanate to provide compounds of formula (8). The reaction is typically performed in a solvent such as but not limited to tetrahydrofuran. Compounds of formula (8) can be reacted with a boronic acid of formula (9A) (or an appropriate boronate ester), wherein R⁵ is as described herein, using Suzuki Coupling conditions known to those skilled in the art and readily available in the literature to provide compounds of formula (9), which are representative of the compounds of this invention.

As shown in Scheme 4, compounds of formula (8), wherein X¹, X², and X³ are as described herein, can be reacted with tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate under Suzuki coupling conditions known to those skilled in the art and widely available in the literature to provide compounds of formula (10). Compounds of formula (11) can be prepared by treating compounds of formula (10) with an acid such as but not limited to trifluoroacetic acid. The reaction is typically performed at room temperature in a solvent such as but not limited to dichloromethane. Compounds of formula (11) can be reacted with compounds of formula (12A) wherein R¹³ is as described herein, in the presence of a carboxyl activating agent such as but not limited to N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, and a coupling agent such but not limited to 1-hydroxybenzotriazole hydrate, to provide compounds of formula (12). The reaction is typically performed at room temperature in a solvent such as but not limited to N,N-dimethylformamide.

Alternatively, compounds of formula (12) can be treated with hydrogen in the presence of palladium on carbon to provide compounds of formula (13). The reaction is typically performed under pressure in a solvent such as but not limited to tetrahydrofuran or N,N-dimethylformamide. Compounds of formula (13) can be reacted with compounds of formula (12A) wherein R¹³ is as described herein, in the presence of a carboxyl activating agent such as but not limited to N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, and a coupling agent such but not limited to 1-hydroxybenzotriazole hydrate, to provide compounds of formula (14). The reaction is typically performed at room temperature in a solvent such as but not limited to N,N-dimethylformamide.

Aqueous potassium hydroxide and a phase transfer catalyst such as but not limited to tetrabutylammonium bromide can be added to a mixture of 4-hydroxy-1-piperidine-1-carboxylic acid tert-butyl ester and 1-fluoro-4-nitrobenzene to provide tert-butyl 4-(4-nitrophenoxy)piperidine-1-carboxylate. tert-Butyl 4-(4-aminophenoxy)piperidine-1-carboxylate can be prepared by reacting tert-butyl 4-(4-nitrophenoxy)piperidine-1-carboxylate with hydrogen in the presence of palladium on carbon. The reaction is typically performed under pressure in a solvent such as but not limited to tetrahydrofuran or N,N-dimethylformamide. tert-Butyl 4-(4-aminophenoxy)piperidine-1-carboxylate can be reacted with bis(2,5-dioxopyrrolidin-1-yl) carbonate and pyridine in acetonitrile, followed by the addition of a base such as but not limited to diisopropylethylamine and compounds of formula (15A) to provide compounds of formula (15). The reaction is typically performed at room temperature. Compounds of formula (16) can be prepared by treating compounds of formula (15) with an acid such as but not limited to trifluoroacetic acid. The reaction is typically performed at room temperature in a solvent such as but not limited to dichloromethane. Compounds of formula (16) can be reacted with compounds of formula (12A) wherein R¹³ is as described herein, in the presence of a carboxyl activating agent such as but not limited to N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride, and a coupling agent such but not limited to 1-hydroxybenzotriazole hydrate, to provide compounds of formula (17). The reaction is typically performed at room temperature in a solvent such as but not limited to N,N-dimethylformamide.

The following examples are presented to provide what is believed to be the most useful and readily understood description of procedures and conceptual aspects of this invention. The exemplified compounds were named using ACD/ChemSketch Version 12.01 (13 May 2009), Advanced Chemistry Development Inc., Toronto, Ontario), or ChemDraw® Ver. 9.0.5 (CambridgeSoft, Cambridge, Mass.). Intermediates were named using ChemDraw® Ver. 9.0.5 (CambridgeSoft, Cambridge, Mass.).

EXPERIMENTALS Example 1 N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 1A Methyl 4-(isoindoline-2-carboxamido)benzoate

Isoindoline (1.693 ml, 14.47 mmol) was dissolved in tetrahydrofuran (20 ml) and cooled to 0° C.; and methyl 4-isocyanatobenzoate (2.18 g, 12.06 mmol) was added by syringe and the resulting mixture was warmed to ambient temperature, and then stirred overnight. The solution was concentrated to a slurry, diluted with ether, and filtered to provide the title compound.

Example 1B 4-(isoindoline-2-carboxamido)benzoic acid

Methyl 4-(isoindoline-2-carboxamido)benzoate (1.65 g, 5.57 mmol) was dissolved in tetrahydrofuran (30 ml) and methanol (15.00 ml) followed by the addition of lithium hydroxide (11.14 ml, 22.27 mmol) and the mixture was allowed to stir at ambient temperature over the weekend. The organic solvent was removed under vacuum, the aqueous layer was adjusted to pH 3 with 2N aqueous HCl, and the resulting solid was filtered with water washes to provide the title compound after drying.

Example 1C N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

4-(Isoindoline-2-carboxamido)benzoic acid (150 mg, 0.531 mmol) and 1-hydroxybenzotriazole hydrate (122 mg, 0.797 mmol) were dissolved in dimethylformamide (3 ml) followed by addition of 3-phenylpropan-1-amine (110 mg, 0.797 mmol) and N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (153 mg, 0.797 mmol). The homogeneous solution was stirred at ambient temperature overnight. The solution was diluted with water to give a precipitate which was filtered, washed with cold ethyl acetate then ether and dried under vacuum to provide the title compound. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.27-8.34 (bs, 1H), 7.93-7.98 (m, 1H), 7.73-7.76 (m, 2H), 7.61-7.64 (m, 2H), 7.32-7.36 (m, 2H), 7.27-7.32 (m, 2H), 7.24-7.28 (m, 2H), 7.19-7.24 (m, 2H), 7.13-7.18 (m, 1H), 4.79 (s, 4H), 3.30 (q, J=6.5 Hz, 2H), 2.65 (t, J=7.6 Hz, 2H), 1.86 (p, J=7.3 Hz, 2H); MS (ESI(+)) m/e 400 (M+H)⁺.

Example 2 N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide Example 2A methyl 4-(5-fluoroisoindoline-2-carboxamido)benzoate

The title compound was prepared as described in Example 1A, substituting 5-fluoroisoindoline for isoindoline.

Example 2B 4-(5-fluoroisoindoline-2-carboxamido)benzoic acid

The title compound was prepared as described in Example 1B, substituting methyl 4-(5-fluoroisoindoline-2-carboxamido)benzoate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 2C tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate

The title compound was prepared as described in Example 1C, substituting 4-(5-fluoroisoindoline-2-carboxamido)benzoic acid for 4-(isoindoline-2-carboxamido)benzoic acid and tert-butyl 4-(aminomethyl)benzylcarbamate for 3-phenylpropan-1-amine.

Example 2D N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide

tert-Butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate (392 mg, 0.756 mmol) was dissolved in dichloromethane, treated with trifluoroacetic acid (582 μl, 7.56 mmol), stirred for 3 hours at ambient temperature and then concentrated to dryness. The resulting solid was triturated with ether, collected and dried under vacuum to provide the title compound. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 4.01 (q, J=5.6 Hz, 2H), 4.46 (d, J=6.0 Hz, 2H), 4.76 (d, J=7.9 Hz, 4H), 7.08-7.29 (m, 2H), 7.32-7.44 (m, 5H), 7.67 (d, J=8.7 Hz, 2H), 7.76-7.86 (m, 2H), 8.12 (s, 2H), 8.63 (s, 1H), 8.91 (t, J=6.2 Hz, 1H); MS (ESI(+)) m/e 419 (M+H)⁺.

TABLE 3 The following Examples were prepared essentially as described in Example 1, substituting the appropriate substituted isoindoline for isoindoline in Example 1A and the appropriate amine for 3-phenylpropan- 1-amine in Example 1C. Some products were purified by flash chromatography while others were purified by reverse-phase HPLC; some compounds also required Boc-deprotection after amide coupling as described in Example 2D. Accordingly, some Examples were isolated as trifluoroacetic acid salts. Ex Name ¹H NMR MS 3 5-cyano-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 8.29 (t, J = 5.6 Hz, 1H), 7.89 (s, 1H), m/e 425 1,3-dihydro-2H- 7.75-7.81 (m, 3H), 7.63-7.68 (m, 2H), 7.59 (M + H)⁺ isoindole-2- (d, J = 8.0 Hz, 1H), 7.15-7.32 (m, 5H), 4.82- carboxamide 4.86 (m, 4H), 3.22-3.30 (m, 2H), 2.63 (t, J = 7.6 Hz, 2H), 1.82 (p, J = 7.4 Hz, 2H) 4 N- ¹H NMR (400 MHz, DMSO-d₆) δ 1.16- (ESI(+)) {4[(cyclopentylmeth- 1.33 (m, 2H), 1.41-1.75 (m, 6H), 2.04- m/e 382 yl)carbamoyl]phenyl}- 2.23 (m, 1H), 3.11-3.22 (m, 2H), 4.76 (d, (M + H)⁺ 5-fluoro-1,3- J = 7.9 Hz, 4H), 7.08-7.19 (m, 1H), 7.24 dihydro-2H- (dd, J = 9.12, 2.4 Hz, 1H), 7.39 (dd, J = 8.3, isoindole-2- 5.16 Hz, 1H), 7.60-7.68 (m, 2H), 7.72- carboxamide 7.82 (m, 2H), 8.27 (t, J = 5.8 Hz, 1H), 8.58 (s, 1 H) 5 5-cyano-N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (ESI(+)) (propylcarbamoyl)phenyl]- (s, 1H), 8.26 (t, J = 5.7 Hz, 1H), 7.89 (s, 1H), m/e 349 1,3-dihydro- 7.79 (dd, J = 8.0, 1.7 Hz, 1H), 7.74-7.79 (m, (M + H)⁺ 2H-isoindole-2- 2H), 7.62-7.67 (m, 2H), 7.59 (d, J = 7.9 Hz, carboxamide 1H), 4.84 (d, J = 7.5 Hz, 4H), 3.14-3.27 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 6 N-(4-{[4-(furo[3,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (ESI(+)) c]pyridin-4- (s, 1H), 8.26 (t, J = 5.7 Hz, 1H), 7.89 (s, 1H), m/e 468 yl)piperazin-1- 7.79 (dd, J = 8.0, 1.7 Hz, 1H), 7.74-7.79 (m, (M + H)⁺ yl]carbonyl}phenyl)- 2H), 7.62-7.67 (m, 2H), 7.59 (d, J = 7.9 Hz, 1,3-dihydro-2H- 1H), 4.84 (d, J = 7.5 Hz, 4H), 3.14-3.27 (m, isoindole-2- 2H), 1.46-1.59 (m, 2H), 0.89 (t, J = 7.4 Hz, carboxamide 3H) 7 5-cyano-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.64 (ESI(−)) (pyridin-2- (s, 1H), 8.13 (dd, J = 5.0, 1.9 Hz, 1H), 7.89 m/e 451 yl)piperazin-1- (s, 1H), 7.79 (d, J = 8.0 Hz, 1H), 7.64-7.68 (M − H)⁻ yl]carbonyl}phenyl)- (m, 2H), 7.51-7.61 (m, 2H), 7.36-7.40 (m, 1,3-dihydro-2H- 2H), 6.85 (d, J = 8.6 Hz, 1H), 6.65-6.69 (m, isoindole-2- 1H), 4.82-4.85 (bs, 4H), 3.48-3.69 (m, 8H) carboxamide 8 5-fluoro-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.93 (ESI(+)) [(pyridin-2- (t, J = 6.0 Hz, 1H), 8.63 (s, 1H), 8.51 (ddd, J = m/e 391 ylmethyl)carbamoyl] 4.8, 1.8, 0.9 Hz, 1H), 7.83-7.87 (m, 2H), (M + H)⁺ phenyl}-1,3-dihydro- 7.75 (td, J = 7.7, 1.8 Hz, 1H), 7.66-7.70 (m, 2H-isoindole-2- 2H), 7.40 (dd, J = 8.4, 5.2 Hz, 1H), 7.22- carboxamide 7.33 (m, 3H), 7.15 (td, J = 8.9, 2.5 Hz, 1H), 4.75-4.80 (m, 4H), 4.55 (d, J = 5.8 Hz, 2H) 9 N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.86 (ESI(+)) (benzylcarbamoyl)phenyl]- (t, J = 6.0 Hz, 1H), 8.61 (s, 1H), 7.80-7.85 m/e 390 5-fluoro-1,3- (m, 2H), 7.64-7.70 (m, 2H), 7.39 (dd, J = (M + H)⁺ dihydro-2H- 8.7, 5.2 Hz, 1H), 7.29-7.35 (m, 4H), 7.20- isoindole-2- 7.28 (m, 2H), 7.15 (ddd, J = 9.4, 8.5, 2.5 Hz, carboxamide 1H), 4.74-4.79 (m, 4H), 4.47 (d, J = 5.9 Hz, 2H) 10 N-{4-[(3,4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) dimethoxybenzyl)carbamoyl]phenyl}- Oxide) δ ppm 7.80-7.82 (m, 2H), 7.64-7.67 m/e 430 1,3-dihydro-2H- (m, 2H), 7.36-7.41 (m, 2H), 7.32-7.35 (m, (M − H)⁻ isoindole-2- 2H), 6.96 (d, J = 1.9 Hz, 1H), 6.91 (d, J = carboxamide 8.2 Hz, 1H), 6.86 (dd, J = 8.2, 2.0 Hz, 1H), 4.79 (s, 4H), 4.39-4.40 (bs, 2H), 3.78 (s, 3H) 11 5-methyl-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.54 (ESI(+)) (pyridin-2- (s, 1H), 8.13 (ddd, J = 4.9, 2.0, 0.8 Hz, 1H), m/e 442 yl)piperazin-1- 7.65-7.68 (m, 2H), 7.55 (ddd, J = 8.6, 7.1, (M + H)⁺ yl]carbonyl}phenyl)- 2.0 Hz, 1H), 7.35-7.39 (m, 2H), 7.25 (d, J = 1,3-dihydro-2H- 7.7 Hz, 1H), 7.17-7.19 (m, 1H), 7.13 (d, J = isoindole-2- 7.8 Hz, 1H), 6.85 (dt, J = 8.6, 0.8 Hz, 1H), carboxamide 6.67 (ddd, J = 7.1, 4.9, 0.8 Hz, 1H), 4.73- 4.75 (bs, 4H), 3.48-3.68 (m, 8H), 2.33 (s, 3H) 12 N-(4-{[4-(thieno[3,2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) c]pyridin-4- (s, 1H), 8.03 (d, J = 5.6 Hz, 1H), 7.78 (d, J = m/e 484 yl)piperazin-1- 5.5 Hz, 1H), 7.64-7.71 (m, 2H), 7.58 (t, J = (M + H)⁺ yl]carbonyl}phenyl)- 5.3 Hz, 2H), 7.30-7.41 (m, 6H), 4.79 (s, 4H), 1,3-dihydro-2H- 3.61-3.94 (m, 4H), 3.39-3.63 (m, 4H) isoindole-2- carboxamide 13 N-{4-[(2,3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethoxybenzyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.30-8.37 (bs, 1H), 8.27- m/e 432 1,3-dihydro-2H- 8.31 (m, 1H), 8.13-8.16 (m, 2H), 7.91-7.93 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.24 (m, 2H), 7.16-7.18 (m, carboxamide 2H), 7.16-7.17 (m, 1H), 6.98 (t, J = 7.8 Hz, 1H), 6.86 (dd, J = 8.1, 1.5 Hz, 1H), 4.91 (d, J = 5.7 Hz, 2H), 4.83-4.85 (m, 4H), 3.85 (s, 3H), 3.71 (s, 3H) 14 5-fluoro-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 8.29 (t, J = 5.5 Hz, 1H), 7.75-7.78 m/e 418 1,3-dihydro-2H- (m, 2H), 7.63-7.67 (m, 2H), 7.39 (dd, J = (M + H)⁺ isoindole-2- 8.5, 5.1 Hz, 1H), 7.11-7.32 (m, 7H), 4.74- carboxamide 4.78 (m, 4H), 3.22-3.31 (m, 2H), 2.63 (t, J = 7.6 Hz, 2H), 1.82 (p, J = 7.4 Hz, 2H) 15 5-fluoro-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58- (ESI(+)) (pyridazin-3- 8.59 (m, 1H), 8.57-8.60 (m, 1H), 7.65-7.69 m/e 447 yl)piperazin-1- (m, 2H), 7.37-7.44 (m, 4H), 7.22-7.29 (m, (M + H)⁺ yl]carbonyl}phenyl)- 2H), 7.15 (td, J = 8.9, 2.5 Hz, 1H), 4.77 (d, J = 1,3-dihydro-2H- 8.3 Hz, 4H), 3.49-3.81 (m, 8H) isoindole-2- carboxamide 16 N-{4-[(2,3-dihydro- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) 1,4-benzodioxin-5- Temp = 90° C.) δ ppm 8.33 (d, J = 1.8 Hz, 1H), m/e 430 ylmethyl)carbamoyl] 8.28-8.29 (bs, 1H), 8.13-8.16 (m, 2H), 7.91- (M + H)⁺ phenyl}-1,3-dihydro- 7.93 (m, 2H), 7.19-7.23 (m, 2H), 7.15-7.19 2H-isoindole-2- (m, 2H), 7.10-7.13 (m, 1H), 6.86 (dd, J = carboxamide 8.1, 1.8 Hz, 1H), 6.80 (dd, J = 8.1, 7.4 Hz, 1H), 4.87 (d, J = 5.7 Hz, 2H), 4.84 (s, 4H), 4.03-4.10 (m, 4H) 17 5-fluoro-N-(4-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.22 (ESI(−)) methylbutyl)-1H- (s, 1H), 8.65 (s, 1H), 8.03 (s, 1H), 7.85-7.89 m/e 434 pyrazol-4- (m, 2H), 7.69-7.73 (m, 2H), 7.56 (d, J = 0.7 (M − H)⁻ yl]carbamoyl}phenyl)- Hz, 1H), 7.40 (dd, J = 8.4, 5.2 Hz, 1H), 7.25 1,3-dihydro-2H- (dd, J = 9.1, 2.4 Hz, 1H), 7.15 (td, J = 8.9, isoindole-2- 2.5 Hz, 1H), 4.73-4.85 (m, 4H), 4.06-4.14 carboxamide (m, 2H), 1.65 (q, J = 7.0 Hz, 2H), 1.40-1.54 (m, 1H), 0.90 (d, J = 6.6 Hz, 6H) 18 N-{4-[(2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (APCI+) fluorobenzyl)carbamoyl]phenyl}- Oxide) δ ppm 8.92 (t, J = 5.9 Hz, 1H), 8.67 m/e 390 1,3-dihydro-2H- (s, 1H), 7.81-7.84 (m, 2H), 7.66-7.68 (m, (M + H)⁺ isoindole-2- 2H), 7.30-7.40 (m, 6H), 7.18 (d, J = 7.2 Hz, carboxamide 1H), 7.16-7.20 (m, 1H), 4.79-4.80 (bs, 4H), 4.52 (d, J = 5.2 Hz, 2H) 19 5-fluoro-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) (pyrimidin-2- (s, 1H), 8.37-8.40 (m, 2H), 7.64-7.68 (m, m/e 447 yl)piperazin-1- 2H), 7.36-7.43 (m, 3H), 7.24 (dd, J = 9.1, 2.4 (M + H)⁺ yl]carbonyl}phenyl)- Hz, 1H), 7.15 (td, J = 8.9, 2.5 Hz, 1H), 6.67 1,3-dihydro-2H- (t, J = 4.7 Hz, 1H), 4.75-4.79 (m, 4H), 3.70- isoindole-2- 3.85 (m, 4H), 3.49-3.69 (m, 4H) carboxamide 20 5-fluoro-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) methylbutyl)carbamoyl]phenyl}- (s, 1H), 8.22 (t, J = 5.6 Hz, 1H), 7.73-7.77 m/e 370 1,3-dihydro-2H- (m, 2H), 7.62-7.66 (m, 2H), 7.39 (dd, J = (M + H)⁺ isoindole-2- 8.4, 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.5 Hz, carboxamide 1H), 7.15 (td, J = 8.9, 2.5 Hz, 1H), 4.74-4.78 (m, 4H), 3.21-3.32 (m, 2H), 1.61 (dp, J = 13.3, 6.6 Hz, 1H), 1.37-1.45 (m, 2H), 0.90 (d, J = 6.6 Hz, 6H) 21 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° (APCI+) methoxybenzyl)carbamoyl]phenyl}- C.) δ ppm 8.27-8.29 (bs, 2H), 8.12-8.14 (m, m/e 402 1,3-dihydro-2H- 2H), 7.90-7.93 (m, 2H), 7.52-7.55 (m, 1H), (M + H)⁺ isoindole-2- 7.19-7.24 (m, 2H), 7.14-7.19 (m, 2H), 6.91 carboxamide (td, J = 7.4, 1.0 Hz, 1H), 6.85 (dd, J = 8.2, 1.1 Hz, 1H), 4.89 (d, J = 5.7 Hz, 2H), 4.83 (s, 4H), 3.65 (s, 3H) 22 5-fluoro-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) (pyridin-2- (s, 1H), 8.10 (dd, J = 5.5, 1.8 Hz, 1H), 7.74- m/e 446 yl)piperazin-1- 7.81 (m, 1H), 7.65-7.69 (m, 2H), 7.37-7.43 (M + H)⁺ yl]carbonyl}phenyl)- (m, 3H), 7.24 (dd, J = 9.1, 2.4 Hz, 1H), 7.07- 1,3-dihydro-2H- 7.19 (m, 2H), 6.82 (t, J = 6.2 Hz, 1H), 4.77 isoindole-2- (d, J = 7.9 Hz, 4H), 3.61-3.69 (bs, 8H) carboxamide 23 N-{4-[(3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) fluorobenzyl)carbamoyl]phenyl}- Oxide) δ ppm 8.99 (t, J = 6.0 Hz, 1H), 7.81- m/e 390 1,3-dihydro-2H- 7.84 (m, 2H), 7.66-7.69 (m, 2H), 7.36-7.46 (M + H)⁺ isoindole-2- (m, 3H), 7.32-7.35 (m, 2H), 7.17 (d, J = 7.7 carboxamide Hz, 1H), 7.12 (dd, J = 10.3, 2.6 Hz, 1H), 7.07 (td, J = 8.5, 2.8 Hz, 1H), 4.79-4.80 (bs, 4H), 4.48 (d, J = 5.8 Hz, 2H) 24 5-fluoro-N-(4-{[3-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) oxopyrrolidin-1- (s, 1H), 8.26 (t, J = 5.6 Hz, 1H), 7.74-7.78 m/e 425 yl)propyl]carbamoyl}phenyl)- (m, 2H), 7.63-7.67 (m, 2H), 7.39 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 8.4, 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.8 Hz, isoindole-2- 1H), 7.15 (ddd, J = 9.4, 8.5, 2.6 Hz, 1H), carboxamide 4.74-4.79 (m, 4H), 3.33-3.38 (m, 2H), 3.16- 3.27 (m, 4H), 2.22 (t, J = 8.0 Hz, 2H), 1.93 (p, J = 7.5 Hz, 2H), 1.69 (p, J = 7.0 Hz, 2H) 25 5-cyano-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (ESI(+)) methylbutyl)carbamoyl]phenyl}- (s, 1H), 8.22 (t, J = 5.6 Hz, 1H), 7.89 (s, 1H), m/e 377 1,3-dihydro-2H- 7.79 (dd, J = 7.9, 1.6 Hz, 1H), 7.73-7.78 (m, (M + H)⁺ isoindole-2- 2H), 7.62-7.67 (m, 2H), 7.59 (d, J = 7.9 Hz, carboxamide 1H), 4.77-4.91 (m, 4H), 3.22-3.32 (m, 2H), 1.53-1.70 (m, 1H), 1.37-1.45 (m, 2H), 0.90 (d, J = 6.6 Hz, 6H) 26 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.54 (ESI(+)) [(cyclopentylmethyl) (s, 1H), 8.26 (t, J = 5.7 Hz, 1H), 7.73-7.78 m/e 378 carbamoyl]phenyl}- (m, 2H), 7.63-7.67 (m, 2H), 7.24 (d, J = 7.7 (M + H)⁺ 5-methyl-1,3- Hz, 1H), 7.17 (s, 1H), 7.11-7.14 (m, 1H), dihydro-2H- 4.73-4.74 (bs, 4H), 3.14-3.19 (m, 2H), 2.33 isoindole-2- (s, 3H), 2.07-2.21 (m, 1H), 1.42-1.75 (m, carboxamide 6H), 1.16-1.34 (m, 2H) 27 N-(4-{[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) cyanophenyl)piperazin-1- Temp = 90° C.) δ ppm 8.34-8.35 (bs, 1H), 7.93- m/e 452 yl]carbonyl}phenyl)- 7.96 (m, 2H), 7.56-7.59 (m, 2H), 7.49-7.52 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.20-7.24 (m, 2H), 7.16-7.19 (m, isoindole-2- 2H), 6.84-6.86 (m, 2H), 4.87 (s, 4H), 3.71- carboxamide 3.74 (m, 4H), 3.24-3.29 (m, 4H) 28 N-{4-[(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) fluorobenzyl)carbamoyl]phenyl}- Oxide) δ ppm 8.95 (t, J = 6.0 Hz, 1H), 7.80- m/e 390 1,3-dihydro-2H- 7.82 (m, 2H), 7.65-7.68 (m, 2H), 7.32-7.40 (M + H)⁺ isoindole-2- (m, 6H), 7.13-7.17 (m, 2H), 4.79-4.80 (bs, carboxamide 4H), 4.45 (d, J = 5.7 Hz, 2H) 29 N-{4-[(3,5- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) dimethoxybenzyl)carbamoyl]phenyl}- Oxide) δ ppm 7.80-7.83 (m, 2H), 7.66-7.69 m/e 492 1,3-dihydro-2H- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.36 (m, (M + H)⁺ isoindole-2- 2H), 6.49 (d, J = 2.3 Hz, 2H), 6.38 (t, J = 2.3 carboxamide Hz, 1H), 4.79-4.80 (bs, 4H), 4.40-4.41 (m, 2H), 3.72 (s, 6H) 30 5-fluoro-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.60 (ESI(+)) [(tetrahydrofuran-3- (s, 1H), 8.39 (t, J = 5.7 Hz, 1H), 7.75-7.79 m/e 383 ylmethyl)carbamoyl] (m, 2H), 7.63-7.68 (m, 2H), 7.40 (dd, J = (M + H)⁺ phenyl}-1,3-dihydro- 8.4, 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.5 Hz, 2H-isoindole-2- 1H), 7.15 (td, J = 8.9, 2.5 Hz, 1H), 4.75-4.79 carboxamide (m, 4H), 3.57-3.78 (m, 3H), 3.48 (dd, J = 8.5, 5.2 Hz, 1H), 3.16-3.30 (m, 2H), 2.40- 2.51 (m, 1H), 1.87-1.99 (m, 1H), 1.54-1.66 (m, 1H) 31 N-{4-[(2,2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethylpropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.28-8.30 (bs, 1H), 8.08- m/e 352 1,3-dihydro-2H- 8.11 (m, 2H), 7.90-7.93 (m, 2H), 7.66-7.71 (M + H)⁺ isoindole-2- (bs, 1H), 7.19-7.23 (m, 2H), 7.15-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 3.41 (d, J = 6.3 Hz, 2H), 0.98 (s, 9H) 32 5-fluoro-N-(4-{[2-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) oxopyrrolidin-1- (s, 1H), 8.31-8.34 (m, 1H), 7.71-7.75 (m, m/e 411 yl)ethyl]carbamoyl}phenyl)- 2H), 7.62-7.66 (m, 2H), 7.39 (dd, J = 8.4, 5.1 (M + H)⁺ 1,3-dihydro- Hz, 1H), 7.24 (dd, J = 9.0, 2.4 Hz, 1H), 7.15 2H-isoindole-2- (td, J = 8.9, 2.5 Hz, 1H), 4.74-4.79 (m, 4H), carboxamide 3.34-3.46 (m, 6H), 2.17 (t, J = 8.0 Hz, 2H), 1.91 (p, J = 7.4 Hz, 2H) 33 N-(4-{[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (trifluoromethoxy)ben- Oxide) δ ppm 7.81-7.83 (m, 2H), 7.66-7.68 m/e 456 zyl]carbamoyl}phenyl)- (m, 2H), 7.43-7.47 (m, 2H), 7.37-7.40 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 7.31-7.35 (m, 4H), 4.79 (s, 4H), 4.49 (s, isoindole-2- 2H) carboxamide 34 N-(4-{[3-fluoro-5- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (trifluoromethyl)ben- Oxide) δ ppm 9.07 (t, J = 6.0 Hz, 1H), 7.81- m/e 458 zyl]carbamoyl}phenyl)- 7.83 (m, 2H), 7.67-7.70 (m, 2H), 7.53-7.56 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.45-7.48 (m, 1H), 7.36-7.41 (m, isoindole-2- 2H), 7.31-7.36 (m, 2H), 4.80 (s, 4H), 4.56 (d, carboxamide J = 5.4 Hz, 2H) 35 5-fluoro-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) (pyrazin-2- (s, 1H), 8.34 (d, J = 1.5 Hz, 1H), 8.10 (dd, J = m/e 447 yl)piperazin-1- 2.6, 1.4 Hz, 1H), 7.87 (d, J = 2.6 Hz, 1H), (M + H)⁺ yl]carbonyl}phenyl)- 7.64-7.68 (m, 2H), 7.36-7.43 (m, 3H), 7.24 1,3-dihydro-2H- (dd, J = 9.1, 2.4 Hz, 1H), 7.11-7.19 (m, 1H), isoindole-2- 4.75-4.79 (m, 4H), 3.58-3.69 (bs, 8H) carboxamide 36 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d_(6,) (ESI(+)) methylbutyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.31 (s, 1H), 7.86-7.89 m/e 352 1,3-dihydro-2H- (m, 1H), 7.72-7.75 (m, 2H), 7.60-7.64 (m, (M + H)⁺ isoindole-2- 2H), 7.28-7.36 (m, 4H), 4.79 (s, 4H), 3.28 (q, carboxamide J = 6.7 Hz, 2H), 1.58-1.71 (m, 1H), 1.45 (q, J = 7.1 Hz, 2H), 0.92 (d, J = 6.6 Hz, 6H) 37 5-methoxy-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 8.29 (t, J = 5.6 Hz, 1H), 7.74-7.79 m/e 429 1,3-dihydro-2H- (m, 2H), 7.63-7.67 (m, 2H), 7.15-7.32 (m, (M + H)⁺ isoindole-2- 6H), 6.94 (d, J = 2.3 Hz, 1H), 6.88 (dd, J = carboxamide 8.3, 2.4 Hz, 1H), 4.65-4.79 (m, 4H), 3.77 (s, 3H), 3.22-3.31 (m, 2H), 2.60-2.68 (m, 2H), 1.77-1.88 (m, 2H) 38 N-{4-[(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) chlorobenzyl)carbamoyl]phenyl}- Oxide) δ ppm 8.97 (t, J = 6.0 Hz, 1H), 8.67 m/e 406 1,3-dihydro-2H- (s, 1H), 7.80-7.83 (m, 2H), 7.66-7.68 (m, (M + H)⁺ isoindole-2- 2H), 7.32-7.40 (m, 8H), 4.79-4.80 (bs, 4H), carboxamide 4.45 (d, J = 5.4 Hz, 2H) 39 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90 (ESI(+)) [(cyclopentylmethyl) C.) δ ppm 8.28-8.29 (bs, 1H), 8.09-8.12 (m, m/e 364 carbamoyl]phenyl}- 2H), 7.90-7.94 (m, 2H), 7.84-7.91 (m, 1H), (M + H)⁺ 1,3-dihydro-2H- 7.19-7.24 (m, 2H), 7.14-7.18 (m, 2H), 4.84 isoindole-2- (s, 4H), 3.51 (dd, J = 7.2, 5.8 Hz, 2H), 2.20- carboxamide 2.32 (m, 1H), 1.67-1.76 (m, 2H), 1.51-1.62 (m, 2H), 1.40-1.51 (m, 2H), 1.27-1.38 (m, 2H) 40 N-{4-[(3,4,5- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) trimethoxybenzyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.59-8.64 (m, 1H), 8.29- m/e 462 1,3-dihydro-2H- 8.32 (m, 1H), 8.17-8.19 (m, 2H), 7.92-7.94 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.24 (m, 2H), 7.15-7.18 (m, carboxamide 2H), 6.82 (s, 2H), 4.84 (s, 4H), 4.77 (d, J = 5.8 Hz, 2H), 3.85 (s, 3H), 3.69 (s, 6H) 41 N-(4-{[4-(pyrimidin- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) 2-yl)piperazin-1- (s, 1H), 8.37-8.40 (m, 2H), 7.66-7.69 (m, m/e 429 yl]carbonyl}phenyl)- 2H), 7.30-7.40 (m, 6H), 6.67 (t, J = 4.7 Hz, (M + H)⁺ 1,3-dihydro-2H- 1H), 4.79 (s, 4H), 3.77-3.81 (m, 4H), 3.58 (s, isoindole-2- 4H) carboxamide 42 5-nitro-N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.68 (ESI(+)) (propylcarbamoyl)phenyl]- (s, 1H), 8.23-8.30 (m, 2H), 8.21 (dd, J = 8.3, m/e 369 1,3-dihydro- 2.4 Hz, 1H), 7.75-7.79 (m, 2H), 7.63-7.67 (M + H)⁺ 2H-isoindole-2- (m, 3H), 4.88-4.91 (m, 4H), 3.16-3.23 (m, carboxamide 2H), 1.46-1.59 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 43 5-methyl-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.54 (ESI(+)) methylbutyl)carbamoyl]phenyl}- (s, 1H), 8.21 (t, J = 5.6 Hz, 1H), 7.73-7.77 m/e 366 1,3-dihydro-2H- (m, 2H), 7.63-7.67 (m, 2H), 7.24 (d, J = 7.7 (M + H)⁺ isoindole-2- Hz, 1H), 7.17 (s, 1H), 7.11-7.14 (m, 1H), carboxamide 4.72-4.74 (bs, 4H), 3.22-3.31 (m, 2H), 2.33 (s, 3H), 1.61 (dp, J = 13.3, 6.6 Hz, 1H), 1.37- 1.45 (m, 2H), 0.90 (d, J = 6.6 Hz, 6H) 44 N-(4-{[4-(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) fluorophenyl)piperazin-1- (s, 1H), 7.65-7.69 (m, 2H), 7.30-7.39 (m, m/e 445 yl]carbonyl}phenyl)- 6H), 6.96-7.14 (m, 4H), 4.78-4.80 (bs, 4H), (M + H)⁺ 1,3-dihydro-2H- 3.52-3.77 (m, 4H), 3.03-3.20 (m, 4H) isoindole-2- carboxamide 45 N-{4-[(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.46-8.51 (bs, 1H), 8.27- m/e 402 1,3-dihydro-2H- 8.29 (bs, 1H), 8.14-8.16 (m, 2H), 7.91-7.93 (M + H)⁺ isoindole-2- (m, 2H), 7.36-7.39 (m, 2H), 7.19-7.23 (m, carboxamide 2H), 7.16-7.18 (m, 2H), 6.88-6.90 (m, 2H), 4.84 (s, 4H), 4.74 (d, J = 5.8 Hz, 2H), 3.65 (s, 3H) 46 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) thienylmethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.73-8.79 (m, 1H), 8.30 m/e 378 1,3-dihydro-2H- (d, J = 2.1 Hz, 1H), 8.11-8.14 (m, 2H), 7.90- (M + H)⁺ isoindole-2- 7.93 (m, 2H), 7.19-7.24 (m, 2H), 7.20-7.21 carboxamide (m, 1H), 7.15-7.18 (m, 2H), 7.05-7.07 (m, 1H), 6.90 (dd, J = 5.0, 3.5 Hz, 1H), 4.94 (d, J = 5.8 Hz, 2H), 4.84 (s, 4H) 47 N-(4-{[4-(pyrimidin- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.64 (ESI(+)) 2-yl)piperazin-1- (s, 1H), 8.37-8.40 (m, 2H), 7.77 (s, 1H), m/e 497 yl]carbonyl}phenyl)- 7.66-7.71 (m, 1H), 7.64-7.69 (m, 2H), 7.61 (M + H)⁺ 5-(trifluoromethyl)- (d, J = 8.1 Hz, 1H), 7.37-7.40 (m, 2H), 6.67 1,3-dihydro-2H- (t, J = 4.7 Hz, 1H), 4.85-4.88 (bs, 4H), 3.73- isoindole-2- 3.87 (m, 4H), 3.50-3.69 (m, 4H) carboxamide 48 N-{4-[(1-ethyl-1H- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.22 (ESI(+)) pyrazol-4- (s, 1H), 8.65 (s, 1H), 8.03 (s, 1H), 7.85-7.89 m/e 394 yl)carbamoyl]phenyl}- (m, 2H), 7.68-7.75 (m, 2H), 7.57 (d, J = 0.7 (M + H)⁺ 5-fluoro-1,3- Hz, 1H), 7.40 (dd, J = 8.4, 5.2 Hz, 1H), 7.25 dihydro-2H- (dd, J = 9.1, 2.5 Hz, 1H), 7.15 (td, J = 8.9, isoindole-2- 2.5 Hz, 1H), 4.71-4.80 (m, 4H), 4.11 (q, J = carboxamide 7.2 Hz, 2H), 1.36 (t, J = 7.2 Hz, 3H) 49 N-{4-[(1-benzyl-1H- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.26 (ESI(+)) pyrazol-4- (s, 1H), 8.65 (s, 1H), 8.11 (d, J = 0.7 Hz, m/e 456 yl)carbamoyl]phenyl}- 1H), 7.84-7.88 (m, 2H), 7.68-7.73 (m, 2H), (M + H)⁺ 5-fluoro-1,3- 7.61 (d, J = 0.7 Hz, 1H), 7.38-7.43 (m, 1H), dihydro-2H- 7.28-7.38 (m, 3H), 7.22-7.27 (m, 3H), 7.11- isoindole-2- 7.19 (m, 1H), 5.31 (s, 2H), 4.70-4.85 (m, 4H) carboxamide 50 N-(4-{[4-(pyridin-2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) yl)piperazin-1- Oxide, Temp = 90° C.) δ ppm 8.08 (ddd, J = m/e 428 yl]carbonyl}phenyl)- 5.4, 1.9, 0.8 Hz, 1H), 7.77 (ddd, J = 8.9, 7.0, (M + H)⁺ 1,3-dihydro-2H- 1.9 Hz, 1H), 7.65-7.68 (m, 2H), 7.38-7.42 isoindole-2- (m, 2H), 7.32-7.39 (m, 4H), 7.03-7.06 (m, carboxamide 1H), 6.83 (ddd, J = 7.0, 5.4, 0.8 Hz, 1H), 4.82 (s, 4H), 3.64-3.72 (m, 8H) 51 N-(4-{[4-(pyrazin-2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) yl)piperazin-1- Oxide) δ ppm 8.33-8.34 (bs, 1H), 8.13-8.14 m/e 429 yl]carbonyl}phenyl)- (bs, 1H), 7.88-7.89 (bs, 1H), 7.65-7.67 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 7.38-7.42 (m, 2H), 7.37-7.40 (m, 2H), isoindole-2- 7.31-7.36 (m, 2H), 4.79-4.80 (bs, 4H), 3.52- carboxamide 3.75 (m, 8H) 52 N-(4-{[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyphenyl)piperazin-1- Temp = 90° C.) δ ppm 8.30-8.32 (bs, 1H), 7.92- m/e 457 yl]carbonyl}phenyl)- 7.96 (m, 2H), 7.56-7.59 (m, 2H), 7.20-7.23 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.16-7.19 (m, 2H), 6.97-7.03 (m, isoindole-2- 1H), 6.90-6.96 (m, 3H), 4.86 (s, 4H), 3.78- carboxamide 3.81 (m, 4H), 3.75 (s, 3H), 3.04-3.07 (m, 4H) 53 N-{4-[(3,3- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) dimethylbutyl)carbamoyl]phenyl}- (s, 1H), 8.20 (t, J = 5.7 Hz, 1H), 7.74-7.76 m/e 366 1,3-dihydro-2H- (m, 2H), 7.64-7.66 (m, 2H), 7.34-7.40 (m, (M + H)⁺ isoindole-2- 2H), 7.29-7.34 (m, 2H), 4.78-4.79 (bs, 4H), carboxamide 3.24-3.28 (m, 2H), 1.43-1.46 (m, 2H), 0.93 (s, 9H) 54 N-(4-{[(2R)- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) tetrahydrofuran-2- Temp = 90° C.) δ ppm 8.33 (d, J = 8.7 Hz, 1H), m/e 366 ylmethyl]carbamoyl} 8.08-8.10 (m, 2H), 7.90-7.96 (bs, 1H), 7.89- (M + H)⁺ phenyl)-1,3-dihydro- 7.93 (m, 2H), 7.19-7.24 (m, 2H), 7.14-7.18 2H-isoindole-2- (m, 2H), 4.84 (s, 4H), 4.10-4.19 (m, 1H), carboxamide 3.74-3.83 (m, 2H), 3.56-3.67 (m, 2H), 1.79- 1.91 (m, 1H), 1.56-1.80 (m, 3H) 55 N-(4-{[4-(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyphenyl)piperazin-1- Temp = 90° C.) δ ppm 8.32-8.33 (bs, 1H), 7.93- m/e 457 yl]carbonyl}phenyl)- 7.96 (m, 2H), 7.55-7.58 (m, 2H), 7.15-7.27 (M + H)⁺ 1,3-dihydro-2H- (m, 5H), 6.63 (t, J = 2.3 Hz, 1H), 6.60 (ddd, isoindole-2- J = 8.2, 2.4, 0.8 Hz, 1H), 6.54 (ddd, J = 8.1, carboxamide 2.3, 0.8 Hz, 1H), 4.86 (s, 4H), 3.72-3.76 (m, 4H), 3.71 (s, 3H), 3.14-3.17 (m, 4H) 56 N-(4-{[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) acetylphenyl)piperazin-1- Temp = 90° C.) δ ppm 8.34 (d, J = 2.2 Hz, 1H), m/e 469 yl]carbonyl}phenyl)- 7.98-8.02 (m, 2H), 7.93-7.96 (m, 2H), 7.56- (M + H)⁺ 1,3-dihydro-2H- 7.60 (m, 2H), 7.20-7.26 (m, 2H), 7.15-7.20 isoindole-2- (m, 2H), 6.89-6.93 (m, 2H), 4.87 (s, 4H), carboxamide 3.73-3.76 (m, 4H), 3.26-3.32 (m, 4H), 2.47 (s, 3H) 57 N-(4-{[2-(2,3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethoxyphenyl)eth- Temp = 90° C.) δ ppm 8.25-8.26 (bs, 1H), 8.08- m/e 446 yl]carbamoyl}phenyl)- 8.13 (bs, 1H), 8.07-8.11 (m, 2H), 7.89-7.92 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.19-7.23 (m, 2H), 7.17-7.19 (m, isoindole-2- 2H), 6.93-6.97 (m, 1H), 6.91 (dd, J = 7.6, 2.0 carboxamide Hz, 1H), 6.82 (dd, J = 7.7, 1.9 Hz, 1H), 4.84 (s, 4H), 3.85-3.89 (m, 2H), 3.83 (s, 3H), 3.70 (s, 3H), 3.11 (t, J = 7.2 Hz, 2H) 58 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) thienylmethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.54-8.60 (m, 1H), 8.27- m/e 378 1,3-dihydro-2H- 8.31 (bs, 1H), 8.12-8.14 (m, 2H), 7.90-7.93 (M + H)⁺ isoindole-2- (m, 2H), 7.26-7.30 (m, 2H), 7.19-7.23 (m, carboxamide 2H), 7.16-7.19 (m, 3H), 4.84 (s, 4H), 4.77 (d, J = 5.8 Hz, 2H) 59 5-methoxy-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (ESI(+)) methylbutyl)carbamoyl]phenyl}- (s, 1H), 8.22 (t, J = 5.6 Hz, 1H), 7.73-7.78 m/e 382 1,3-dihydro-2H- (m, 2H), 7.62-7.67 (m, 2H), 7.26 (d, J = 8.3 (M + H)⁺ isoindole-2- Hz, 1H), 6.94 (d, J = 2.0 Hz, 1H), 6.89 (dd, J = carboxamide 8.3, 2.4 Hz, 1H), 4.70-4.75 (m, 4H), 3.77 (s, 3H), 3.22-3.30 (m, 2H), 1.53-1.69 (m, 1H), 1.37-1.45 (m, 2H), 0.91 (d, J = 6.6 Hz, 6H) 60 N-{4-[(pyridin-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.93 (ESI(+)) ylmethyl)carbamoyl] (t, J = 6.0 Hz, 1H), 8.61 (s, 1H), 8.51 (ddd, J = m/e 372 phenyl}-1,3-dihydro- 4.8, 1.8, 0.9 Hz, 1H), 7.83-7.87 (m, 2H), (M + H)⁺ 2H-isoindole-2- 7.75 (td, J = 7.7, 1.8 Hz, 1H), 7.67-7.72 (m, carboxamide 2H), 7.29-7.40 (m, 5H), 7.26 (ddd, J = 7.5, 4.8, 1.1 Hz, 1H), 4.80 (s, 4H), 4.56 (d, J = 5.8 Hz, 2H) 61 5-fluoro-N-(4-{[2-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.60 (ESI(+)) thienyl)ethyl]carbamoyl}phenyl)- (s, 1H), 8.45 (t, J = 5.6 Hz, 1H), 7.74-7.78 m/e 410 1,3-dihydro-2H- (m, 2H), 7.63-7.67 (m, 2H), 7.40 (dd, J = (M + H)⁺ isoindole-2- 8.4, 5.2 Hz, 1H), 7.33 (dd, J = 5.0, 1.3 Hz, carboxamide 1H), 7.24 (dd, J = 9.1, 2.3 Hz, 1H), 7.10- 7.19 (m, 1H), 6.96 (dd, J = 5.0, 3.4 Hz, 1H), 6.90-6.93 (m, 1H), 4.71-4.84 (m, 4H), 3.44- 3.53 (m, 2H), 3.06 (t, J = 7.2 Hz, 2H) 62 N-(4-{[(2S)- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) tetrahydrofuran-2- Temp = 90° C.) δ ppm 8.27-8.31 (bs, 1H), 8.06- m/e 366 ylmethyl]carbamoyl} 8.12 (m, 2H), 7.89-7.93 (m, 2H), 7.89-7.92 (M + H)⁺ phenyl)-1,3-dihydro- (m, 1H), 7.18-7.25 (m, 2H), 7.14-7.19 (m, 2H-isoindole-2- 2H), 4.84 (s, 4H), 4.14 (qd, J = 6.7, 4.5 Hz, carboxamide 1H), 3.73-3.83 (m, 2H), 3.55-3.68 (m, 2H), 1.80-1.91 (m, 1H), 1.56-1.79 (m, 3H) 63 N-(4-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.21 (ESI(+)) methylbutyl)-1H- (s, 1H), 8.63 (s, 1H), 8.03 (d, J = 0.7 Hz, m/e 418 pyrazol-4- 1H), 7.85-7.89 (m, 2H), 7.70-7.74 (m, 2H), (M + H)⁺ yl]carbamoyl}phenyl)- 7.56 (d, J = 0.7 Hz, 1H), 7.30-7.40 (m, 4H), 1,3-dihydro-2H- 4.80 (s, 4H), 4.10 (t, J = 7.1 Hz, 2H), 1.65 isoindole-2- (q, J = 7.0 Hz, 2H), 1.40-1.56 (m, 1H), 0.90 carboxamide (d, J = 6.6 Hz, 6H) 64 4-chloro-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.66 (ESI(+)) (pyridin-2- (s, 1H), 8.13 (dd, J = 4.9, 1.9 Hz, 1H), 7.64- m/e 462 yl)piperazin-1- 7.71 (m, 2H), 7.56 (ddd, J = 8.7, 7.0, 1.9 Hz, (M + H)⁺ yl]carbonyl}phenyl)- 1H), 7.34-7.41 (m, 5H), 6.85 (d, J = 8.6 Hz, 1,3-dihydro-2H- 1H), 6.67 (dd, J = 6.9, 4.8 Hz, 1H), 4.76- isoindole-2- 4.92 (m, 4H), 3.45-3.74 (m, 8H) carboxamide 65 N-{4-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) phenylpiperazin-1- (s, 1H), 7.65-7.69 (m, 2H), 7.29-7.41 (m, m/e 427 yl)carbonyl]phenyl}- 6H), 7.18-7.27 (m, 2H), 6.94-6.98 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 6.81 (t, J = 7.3 Hz, 1H), 4.79-4.80 (bs, 4H), isoindole-2- 3.58-3.74 (m, 4H), 3.14-3.22 (m, 4H) carboxamide 66 N-{4-[(6- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) aminohexyl)carbamoyl]phenyl}- (s, 1H), 8.26 (t, J = 5.6 Hz, 1H), 7.73-7.80 m/e 381 1,3-dihydro-2H- (m, 2H), 7.64-7.68 (m, 2H), 7.61-7.69 (m, (M + H)⁺ isoindole-2- 2H), 7.30-7.39 (m, 4H), 4.79 (s, 4H), 3.21- carboxamide 3.26 (m, 2H), 2.72-2.84 (m, 2H), 1.48-1.57 (m, 4H), 1.31-1.35 (m, 4H) 67 4-chloro-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.66 (ESI(+)) methylbutyl)carbamoyl]phenyl}- (s, 1H), 8.22 (t, J = 5.6 Hz, 1H), 7.74-7.78 m/e 386 1,3-dihydro-2H- (m, 2H), 7.63-7.68 (m, 2H), 7.35-7.42 (m, (M + H)⁺ isoindole-2- 3H), 4.76-4.92 (m, 4H), 3.22-3.30 (m, 2H), carboxamide 1.54-1.68 (m, 1H), 1.37-1.45 (m, 2H), 0.91 (d, J = 6.6 Hz, 6H) 68 N-(4-{[2-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) thienyl)ethyl]carbamoyl}phenyl)- (s, 1H), 8.45 (t, J = 5.6 Hz, 1H), 7.75-7.78 m/e 390 1,3-dihydro-2H- (m, 2H), 7.65-7.68 (m, 2H), 7.25-7.44 (m, (M + H)⁺ isoindole-2- 5H), 6.96 (dd, J = 5.1, 3.4 Hz, 1H), 6.90- carboxamide 6.93 (m, 1H), 4.78-4.79 (bs, 4H), 3.45-3.52 (m, 2H), 3.06 (t, J = 7.2 Hz, 2H) 69 5-methoxy-N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) (pyridin-2- (s, 1H), 8.10 (dd, J = 5.5, 1.8 Hz, 1H), 7.75- m/e 458 yl)piperazin-1- 7.82 (m, 1H), 7.65-7.69 (m, 2H), 7.37-7.41 (M + H)⁺ yl]carbonyl}phenyl)- (m, 2H), 7.27 (d, J = 8.3 Hz, 1H), 7.08-7.12 1,3-dihydro-2H- (m, 1H), 6.95 (d, J = 2.3 Hz, 1H), 6.89 (dd, J = isoindole-2- 8.3, 2.4 Hz, 1H), 6.82 (t, J = 6.2 Hz, 1H), carboxamide 4.71-4.75 (m, 4H), 3.95-4.67 (m, 8H), 3.77 (s, 3H) 70 N-{4-[(1,3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) benzodioxol-5- Oxide) δ ppm 7.79-7.81 (m, 2H), 7.65-7.67 m/e 416 ylmethyl)carbamoyl] (m, 2H), 7.32-7.39 (m, 4H), 6.89 (d, J = 1.6 (M + H)⁺ phenyl}-1,3-dihydro- Hz, 1H), 6.86 (d, J = 7.9 Hz, 1H), 6.81 (dd, J = 2H-isoindole-2- 8.0, 1.4 Hz, 1H), 5.97 (s, 2H), 4.79 (s, 4H), carboxamide 4.37(d, J = 5.2 Hz, 2H) 71 N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.83 (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- (t, J = 6.0 Hz, 1 H), 8.59 (s, 1 H), 7.77-7.87 m/e 402 1,3-dihydro-2H- (m, 2 H), 7.68 (d, J = 8.7 Hz, 2 H), 7.28-7.42 (M + H)⁺ isoindole-2- (m, 4 H), 7.24 (t, J = 8.1 Hz, 1 H), 6.75-6.94 carboxamide (m, 3 H), 4.79 (s, 4 H), 4.43 (d, J = 6.0 Hz, 2 H), 3.73 (s, 3 H) 72 N-(4-{[4-(pyridin-3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) yl)piperazin-1- (s, 1H), 8.33 (d, J = 2.9 Hz, 1H), 8.03 (dd, J = m/e 428 yl]carbonyl}phenyl)- 4.5, 1.3 Hz, 1H), 7.66-7.69 (m, 2H), 7.30- (M + H)⁺ 1,3-dihydro-2H- 7.41 (m, 7H), 7.24 (dd, J = 8.4, 4.5 Hz, 1H), isoindole-2- 4.79 (s, 4H), 3.64-3.67 (m, 4H), 3.21-3.29 carboxamide (m, 4H) 73 N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.86 (ESI(+)) (benzylcarbamoyl)phenyl]- (t, J = 6.0 Hz, 1H), 8.59 (s, 1H), 7.80-7.84 m/e 372 1,3-dihydro- (m, 2H), 7.66-7.70 (m, 2H), 7.31-7.36 (m, (M + H)⁺ 2H-isoindole-2- 9H), 4.79 (s, 4H), 4.47 (d, J = 5.9 Hz, 2H) carboxamide 74 N-(4-{[4-(pyridazin- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56- (ESI(−)) 3-yl)piperazin-1- 8.60 (m, 1H), 8.57-8.58 (m, 1H), 7.64-7.72 m/e 427 yl]carbonyl}phenyl)- (m, 2H), 7.24-7.45 (m, 8H), 4.80 (s, 4H), (M − H)⁻ 1,3-dihydro-2H- 3.60-3.70 (m, 8H) isoindole-2- carboxamide 75 N-{4-[(pyrimidin-4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) ylmethyl)carbamoyl] Temp = 90° C.) δ ppm 9.21 (d, J = 1.4 Hz, 1H), m/e 372 phenyl}-1,3-dihydro- 8.86-8.90 (m, 1H), 8.61 (d, J = 5.1 Hz, 1H), (M − H)⁻ 2H-isoindole-2- 8.34-8.36 (bs, 1H), 8.17-8.20 (m, 2H), 7.95- carboxamide 7.97 (m, 2H), 7.41-7.43 (m, 1H), 7.20-7.23 (m, 2H), 7.15-7.19 (m, 2H), 4.87 (d, J = 5.8 Hz, 2H), 4.85 (s, 4H) 76 N-(4-{[4-(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(−)) fluorophenyl)piperazin-1- (s, 1H), 7.65-7.69 (m, 2H), 7.15-7.46 (m, m/e 443 yl]carbonyl}phenyl)- 7H), 6.70-6.84 (m, 2H), 6.54-6.61 (m, 1H), (M − H)⁻ 1,3-dihydro-2H- 4.79-4.80 (bs, 4H), 3.54-3.75 (m, 4H), 3.12- isoindole-2- 3.28 (m, 4H) carboxamide 77 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylbutyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.28-8.30 (bs, 1H), 8.09- m/e 352 1,3-dihydro-2H- 8.12 (m, 2H), 7.90-7.93 (m, 2H), 7.84 (d, J = (M + H)⁺ isoindole-2- 6.2 Hz, 1H), 7.16-7.26 (m, 4H), 4.84 (s, 4H), carboxamide 3.51 (dt, J = 13.2, 6.1 Hz, 1H), 3.39 (ddd, J = 13.2, 7.1, 6.0 Hz, 1H), 1.71-1.83 (m, 1H), 1.42-1.53 (m, 1H), 1.08-1.24 (m, 1H), 0.93 (d, J = 6.7 Hz, 3H), 0.86 (t, J = 7.4 Hz, 3H) 78 N-(4-{[4-(pyridin-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (ESI(+)) yl)piperazin-1- (s, 1H), 8.10 (dd, J = 5.5, 1.8 Hz, 1H), 7.46- m/e 496 yl]carbonyl}phenyl)- 7.82 (m, 6H), 7.38-7.42 (m, 2H), 7.06-7.10 (M + H)⁺ 5-(trifluoromethyl)- (m, 1H), 6.81 (t, J = 6.2 Hz, 1H), 4.85-4.88 1,3-dihydro-2H- (bs, 4H), 3.56-3.73 (bs, 8H) isoindole-2- carboxamide 79 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) butoxypropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.27-8.29 (bs, 1H), 8.07- m/e 394 1,3-dihydro-2H- 8.10 (m, 2H), 7.93-7.98 (m, 1H), 7.90-7.94 (M − H)⁻ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.16-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 3.69 (td, J = 6.7, 5.6 Hz, 2H), 3.51 (t, J = 6.1 Hz, 2H), 3.36 (t, J = 6.5 Hz, 2H), 1.95 (p, J = 6.4 Hz, 2H), 1.44-1.60 (m, 2H), 1.25-1.42 (m, 2H), 0.85 (t, J = 7.3 Hz, 3H) 80 N-(4-{[(1S)-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxy-1- Temp = 90° C.) δ ppm 8.28-8.30 (bs, 1H), 8.14- m/e 402 phenylethyl]carbamoyl}phenyl)- 8.18 (m, 1H), 8.07-8.11 (m, 2H), 7.87-7.89 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.60-7.65 (m, 2H), 7.26-7.32 (m, isoindole-2- 2H), 7.20-7.23 (m, 3H), 7.14-7.18 (m, 3H), carboxamide 5.67-5.73 (m, 1H), 4.83 (s, 4H), 4.21-4.25 (m, 2H) 81 N-(4-{[2-(3,4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) dihydroxyphenyl)eth- Oxide) δ ppm 7.74-7.76 (m, 2H), 7.64-7.67 m/e 418 yl]carbamoyl}phenyl)- (m, 2H), 7.32-7.40 (m, 4H), 6.66 (d, J = 10.7 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 6.66 (d, J = 2.4 Hz, 1H), 6.51 (dd, J = isoindole-2- 8.0, 2.1 Hz, 1H), 4.79-4.80 (bs, 4H), 3.39 carboxamide (t, J = 7.5 Hz, 2H), 2.66 (t, J = 7.5 Hz, 2H) 82 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) propoxypropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.28-8.30 (bs, 1H), 8.07- m/e 380 1,3-dihydro-2H- 8.10 (m, 2H), 7.93-8.00 (m, 1H), 7.90-7.94 (M − H)⁻ isoindole-2- (m, 2H), 7.19-7.24 (m, 2H), 7.15-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 3.66-3.71 (m, 2H), 3.51 (t, J = 6.1 Hz, 2H), 3.30 (t, J = 6.5 Hz, 2H), 1.94 (p, J = 6.4 Hz, 2H), 1.48-1.57 (m, 2H), 0.85 (t, J = 7.4 Hz, 3H) 83 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) furylmethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.37-8.53 (m, 1H), 8.28- m/e 362 1,3-dihydro-2H- 8.31 (bs, 1H), 8.10-8.13 (m, 2H), 7.90-7.93 (M + H)⁺ isoindole-2- (m, 2H), 7.52-7.54 (m, 1H), 7.41 (t, J = 1.7 carboxamide Hz, 1H), 7.19-7.23 (m, 2H), 7.15-7.18 (m, 2H), 6.51-6.53 (m, 1H), 4.84 (s, 4H), 4.60- 4.62 (m, 2H) 84 N-(4-{[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) cyanophenyl)piperazin-1- Temp = 90° C.) δ ppm 8.32-8.33 (bs, 1H), 7.92- m/e 452 yl]carbonyl}phenyl)- 7.95 (m, 2H), 7.55-7.58 (m, 1H), 7.53-7.59 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.39-7.44 (m, 1H), 7.20-7.25 (m, isoindole-2- 2H), 7.15-7.20 (m, 2H), 6.93-6.99 (m, 2H), carboxamide 4.80-4.87 (m, 4H), 3.80-3.83 (m, 4H), 3.15- 3.17 (m, 4H) 85 N-{4-[(3-hydroxy-2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) methylphenyl)carbamoyl]phenyl}- Oxide) δ ppm 7.89-7.92 (m, 2H), 7.69-7.72 m/e 386 1,3-dihydro-2H- (m, 2H), 7.38-7.41 (m, 2H), 7.33-7.36 (m, (M − H)⁻ isoindole-2- 2H), 7.02 (t, J = 7.9 Hz, 1H), 6.79 (d, J = 7.8 carboxamide Hz, 1H), 6.74 (d, J = 8.0 Hz, 1H), 4.80-4.82 (bs, 4H), 2.02 (s, 3H) 86 N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.64 (ESI(+)) methylbutyl)carbamoyl]phenyl}- (s, 1H), 8.21 (t, J = 5.6 Hz, 1H), 7.74-7.78 m/e 420 5-(trifluoromethyl)-1,3- (m, 3H), 7.56-7.70 (m, 4H), 4.85-4.87 (bs, (M + H)⁺ dihydro-2H- 4H), 3.22-3.30 (m, 2H), 1.51-1.72 (m, 1H), isoindole-2- 1.37-1.45 (m, 2H), 0.91 (d, J = 6.6 Hz, 6H) carboxamide 87 N-{4-[(3-methyl-1H- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) indazol-5- Temp = 90° C.) δ ppm 10.02-10.04 (bs, 1H), m/e 412 yl)carbamoyl]phenyl}- 8.41-8.42 (m, 1H), 8.33-8.35 (bs, 1H), 8.23- (M + H)⁺ 1,3-dihydro-2H- 8.26 (m, 2H), 7.95-7.98 (m, 2H), 7.86 (dd, J = isoindole-2- 8.8, 1.9 Hz, 1H), 7.48-7.53 (m, 1H), 7.20- carboxamide 7.25 (m, 2H), 7.15-7.19 (m, 2H), 4.86 (s, 4H), 2.58 (s, 3H) 88 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) ethoxypropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.27-8.28 (bs, 1H), 8.07- m/e 368 1,3-dihydro-2H- 8.10 (m, 2H), 7.94-7.99 (m, 1H), 7.89-7.94 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.15-7.19 (m, carboxamide 2H), 4.84 (s, 4H), 3.68 (td, J = 6.7, 5.7 Hz, 2H), 3.49 (t, J = 6.1 Hz, 2H), 3.38 (q, J = 6.9 Hz, 2H), 1.93 (p, J = 6.4 Hz, 2H), 1.10 (t, J = 6.9 Hz, 3H) 89 N-(4-{[4-(pyrazin-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (ESI(−)) yl)piperazin-1- (s, 1H), 8.34 (s, 1H), 8.09-8.12 (bs, 1H), 7.87 m/e 495 yl]carbonyl}phenyl)- (d, J = 2.6 Hz, 1H), 7.76-7.78 (bs, 1H), 7.64- (M − H)⁻ 5-(trifluoromethyl)- 7.73 (m, 3H), 7.58-7.64 (m, 1H), 7.37-7.41 1,3-dihydro-2H- (m, 2H), 4.85-4.88 (bs, 4H), 3.62-3.65 (m, isoindole-2- 8H) carboxamide 90 N-(4-{[2-(2,5- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) dimethoxyphenyl)eth- Oxide) δ ppm 7.73-7.75 (m, 2H), 7.62-7.65 m/e 444 yl]carbamoyl}phenyl)- (m, 2H), 7.37-7.40 (m, 2H), 7.32-7.35 (m, (M − H)⁻ 1,3-dihydro-2H- 2H), 6.90 (d, J = 8.6 Hz, 1H), 6.76-6.78 (m, isoindole-2- 2H), 4.78-4.80 (bs, 4H), 3.78 (s, 3H), 3.44 (t, carboxamide J = 7.3 Hz, 2H), 2.81 (t, J = 7.2 Hz, 2H) 91 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) [(tetrahydrofuran-3- (s, 1H), 8.39 (t, J = 5.7 Hz, 1H), 7.75-7.79 m/e 366 ylmethyl)carbamoyl] (m, 2H), 7.65-7.68 (m, 2H), 7.30-7.39 (m, (M + H)⁺ phenyl}-1,3-dihydro- 4H), 4.79 (s, 4H), 3.57-3.78 (m, 3H), 3.48 2H-isoindole-2- (dd, J = 8.5, 5.2 Hz, 1H), 3.17-3.28 (m, 2H), carboxamide 2.41-2.51 (m, 1H), 1.93 (dtd, J = 12.2, 8.0, 5.7 Hz, 1H), 1.54-1.66 (m, 1H) 92 N-{4-[(1-benzyl-1H- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.25 (ESI(+)) pyrazol-4- (s, 1H), 8.63 (s, 1H), 8.11 (s, 1H), 7.84-7.88 m/e 438 yl)carbamoyl]phenyl}- (m, 2H), 7.70-7.74 (m, 2H), 7.61 (d, J = 0.7 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 7.23-7.40 (m, 9H), 5.31 (s, 2H), isoindole-2- 4.79-4.80 (bs, 4H) carboxamide 93 methyl 5-({4-[(1,3- ¹H NMR (400 MHz, Pyridine-d₅, (APCI(+)) dihydro-2H-isoindol- Temp = 90° C.) δ ppm 10.25-10.26 (bs, 1H), m/e 456 2-ylcarbonyl)amino]ben- 8.92 (d, J = 1.9 Hz, 1H), 8.34-8.36 (bs, 1H), (M + H)⁺ zoyl}amino)-1H- 8.23-8.25 (m, 2H), 8.17 (dd, J = 8.9, 2.0 Hz, indazole-3- 1H), 7.95-7.98 (m, 2H), 7.64 (d, J = 8.9 Hz, carboxylate 1H), 7.20-7.24 (m, 2H), 7.15-7.20 (m, 2H), 4.86 (s, 4H), 3.90 (s, 3H) 94 N-(4-{[2-(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) oxopyrrolidin-1- Oxide, Temp = 90° C.) δ ppm 7.73-7.75 (m, m/e 393 yl)ethyl]carbamoyl}phenyl)- 2H), 7.62-7.65 (m, 2H), 7.32-7.40 (m, 4H), (M + H)⁺ 1,3-dihydro- 4.82 (s, 4H), 3.38-3.47 (m, 6H), 2.23 (t, J = 2H-isoindole-2- 8.0 Hz, 2H), 1.91-1.99 (m, 2H) carboxamide 95 N-{4-[(pyridin-4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) ylmethyl)carbamoyl] Temp = 90° C.) δ ppm 8.81-8.88 (m, 1H), 8.57- m/e 373 phenyl}-1,3-dihydro- 8.60 (m, 2H), 8.34-8.37 (bs, 1H), 8.16-8.19 (M + H)⁺ 2H-isoindole-2- (m, 2H), 7.94-7.98 (m, 2H), 7.30-7.32 (m, carboxamide 2H), 7.19-7.23 (m, 2H), 7.17-7.19 (m, 2H), 4.85 (s, 4H), 4.74 (d, J = 6.0 Hz, 2H) 96 N-(4-{[4-(5- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) chloropyridin-2- (s, 1H), 8.13 (d, J = 2.7 Hz, 1H), 7.64-7.70 m/e 462 yl)piperazin-1- (m, 2H), 7.63 (dd, J = 9.2, 2.7 Hz, 1H), 7.30- (M + H)⁺ yl]carbonyl}phenyl)- 7.39 (m, 6H), 6.90 (d, J = 9.1 Hz, 1H), 4.79- 1,3-dihydro-2H- 4.80 (bs, 4H), 3.47-3.72 (m, 8H) isoindole-2- carboxamide 97 N-(4-{[2-(1H-indol-3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) yl)ethyl]carbamoyl}phenyl)- Oxide, Temp = 90° C.) δ ppm 7.75-7.78 (m, m/e 425 1,3-dihydro- 2H), 7.63-7.66 (m, 2H), 7.59-7.63 (m, 1H), (M + H)⁺ 2H-isoindole-2- 7.32-7.40 (m, 5H), 7.17 (s, 1H), 7.10 (ddd, J = carboxamide 8.1, 6.9, 1.2 Hz, 1H), 7.01 (ddd, J = 7.9, 6.9, 1.0 Hz, 1H), 4.82 (s, 4H), 3.60 (t, J = 7.4 Hz, 2H), 3.01 (t, J = 7.4 Hz, 2H) 98 N-(4-{[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (trifluoromethyl)ben- Oxide) δ ppm 9.05 (t, J = 6.0 Hz, 1H), 7.81- m/e 440 zyl]carbamoyl}phenyl)- 7.84 (m, 2H), 7.66-7.71 (m, 4H), 7.53-7.55 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.36-7.41 (m, 2H), 7.32-7.36 (m, isoindole-2- 2H), 4.79-4.80 (bs, 4H), 4.54-4.56 (m, 2H) carboxamide 99 N-{4-[(3,5- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (APCI(+)) dimethoxyphenyl)carbamoyl]phenyl}- Oxide) δ ppm 7.88-7.91 (m, 2H), 7.71-7.74 m/e 418 1,3-dihydro-2H- (m, 2H), 7.38-7.41 (m, 2H), 7.33-7.36 (m, (M + H)⁺ isoindole-2- 2H), 7.06-7.07 (m, 2H), 6.27 (t, J = 2.2 Hz, carboxamide 1H), 4.80-4.81 (bs, 4H), 3.78 (s, 6H) 100 N-{4-[(pyridin-3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) ylmethyl)carbamoyl] Temp = 90° C.) δ ppm 8.81 (d, J = 2.3 Hz, 1H), m/e 373 phenyl}-1,3-dihydro- 8.75-8.80 (m, 1H), 8.53 (dd, J = 4.7, 1.6 Hz, (M + H)⁺ 2H-isoindole-2- 1H), 8.31-8.33 (bs, 1H), 8.12-8.15 (m, 2H), carboxamide 7.91-7.94 (m, 2H), 7.71-7.75 (m, 1H), 7.19- 7.23 (m, 2H), 7.16-7.18 (m, 2H), 7.10-7.14 (m, 1H), 4.84 (s, 4H), 4.75 (d, J = 5.8 Hz, 2H) 101 N-[4-(2,3-dihydro- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) 1,4-benzodioxin-6- Temp = 90° C.) δ ppm 9.88-9.89 (bs, 1H), 8.30 m/e 416 ylcarbamoyl)phenyl]- (d, J = 2.0 Hz, 1H), 8.13-8.16 (m, 2H), 7.89- (M + H)⁺ 1,3-dihydro-2H- 7.92 (m, 2H), 7.77 (d, J = 2.5 Hz, 1H), 7.41 isoindole-2- (dd, J = 8.6, 2.5 Hz, 1H), 7.19-7.23 (m, 2H), carboxamide 7.17-7.19 (m, 2H), 6.93 (d, J = 8.6 Hz, 1H), 4.84 (s, 4H), 4.07-4.10 (m, 4H) 102 N-(4-{[4-(2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) fluorobenzoyl)piperazin-1- Oxide) δ ppm 7.63-7.65 (m, 2H), 7.50-7.57 m/e 473 yl]carbonyl}phenyl)- (m, 1H), 7.42-7.46 (m, 1H), 7.35-7.41 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 7.28-7.35 (m, 4H), 4.78-4.79 (bs, 4H), isoindole-2- 3.71-3.76 (m, 2H), 3.51-3.62 (m, 4H), 3.30- carboxamide 3.33 (m, 2H) 103 N-(4-{[2-(5- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) methoxy-1H-indol-3- Oxide, Temp = 90° C.) δ ppm 7.75-7.78 (m, m/e 455 yl)ethyl]carbamoyl}phenyl)- 2H), 7.62-7.65 (m, 2H), 7.36-7.41 (m, 2H), (M + H)⁺ 1,3-dihydro- 7.31-7.36 (m, 2H), 7.27 (dd, J = 8.7, 0.6 Hz, 2H-isoindole-2- 1H), 7.14 (q, J = 0.7 Hz, 1H), 7.11 (dd, J = carboxamide 2.4, 0.5 Hz, 1H), 6.76 (dd, J = 8.6, 2.4 Hz, 1H), 4.82 (s, 4H), 3.78 (s, 3H), 3.58 (t, J = 7.3 Hz, 2H), 2.97 (t, J = 7.3 Hz, 2H) 104 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (APCI(+)) aminobenzyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.39-8.43 (m, 1H), 8.30- m/e 387 1,3-dihydro-2H- 8.32 (bs, 1H), 8.11-8.14 (m, 2H), 7.90-7.93 (M + H)⁺ isoindole-2- (m, 2H), 7.20-7.24 (m, 2H), 7.17-7.19 (m, carboxamide 2H), 7.09 (t, J = 7.7 Hz, 1H), 6.92 (t, J = 1.9 Hz, 1H), 6.80 (dd, J = 7.5, 1.4 Hz, 1H), 6.67- 6.70 (m, 1H), 4.85 (s, 4H), 4.73 (d, J = 5.8 Hz, 2H) 105 N-(4-{[2-(2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) chlorophenyl)ethyl]carbamoyl}phenyl)- Oxide) δ ppm 8.49 (t, J = 5.6 Hz, 1H), 7.73- m/e 420 1,3-dihydro-2H- 7.75 (m, 2H), 7.63-7.65 (m, 2H), 7.43 (dd, J = (M + H)⁺ isoindole-2- 7.4, 1.9 Hz, 1H), 7.36-7.40 (m, 2H), 7.35- carboxamide 7.37 (m, 1H), 7.32-7.36 (m, 2H), 7.24-7.31 (m, 1H), 4.78-4.80 (bs, 4H), 3.49-3.54 (m, 2H), 2.98 (t, J = 7.2 Hz, 2H) 106 N-(4-{[(2R)-1- ¹H NMR (300 MHz, DMSO-d₆) d ppm 8.56 (ESI(+)) hydroxy-4- (s, 1 H) 7.71-7.86 (m, 3H) 7.59-7.71 (m, m/e 382 methylpentan-2- 2H) 7.20-7.45 (m, 4H) 4.79 (s, 4H) 4.64 (M + H)⁺ yl]carbamoyl}phenyl)- (t, J = 5.8 Hz, 1H) 3.90-4.16 (m, 1H) 3.21- 1,3-dihydro-2H- 3.52 (m, 2H) 1.54-1.72 (m, 1H) 1.28- isoindole-2- 1.53 (m, 2H) 0.88 (t, J = 6.7 Hz, 6H) carboxamide 107 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) propoxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 8.08- m/e 368 1,3-dihydro-2H- 8.11 (m, 2H), 7.99-8.06 (m, 1H), 7.89-7.92 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.16-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 3.77 (q, J = 5.7 Hz, 2H), 3.65 (t, J = 5.7 Hz, 2H), 3.35 (t, J = 6.5 Hz, 2H), 1.43-1.59 (m, 2H), 0.84 (t, J = 7.4 Hz, 3H) 108 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) isobutoxypropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.27-8.29 (bs, 1H), 8.08- m/e 396 1,3-dihydro-2H- 8.10 (m, 2H), 7.92-7.98 (m, 1H), 7.90-7.94 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.16-7.19 (m, carboxamide 2H), 4.84 (s, 4H), 3.66-3.72 (m, 2H), 3.51 (t, J = 6.1 Hz, 2H), 3.13 (d, J = 6.4 Hz, 2H), 1.95 (p, J = 6.4 Hz, 2H), 1.75-1.87 (m, 1H), 0.87 (d, J = 6.7 Hz, 6H) 109 N-(4-{[4-(pyridin-4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) yl)piperazin-1- (s, 1H), 8.16-8.20 (m, 2H), 7.65-7.69 (m, m/e 428 yl]carbonyl}phenyl)- 2H), 7.30-7.40 (m, 6H), 6.81-6.85 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 4.79-4.80 (bs, 4H), 3.60-3.64 (m, 4H) isoindole-2- carboxamide 110 N-[4-({4-[5- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) (trifluoromethyl)pyridin- Oxide) δ ppm 8.42-8.43 (m, 1H), 7.83 (dd, J = m/e 494 2-yl]piperazin-1- 9.1, 2.6 Hz, 1H), 7.65-7.67 (m, 2H), 7.38- (M − H)⁻ yl}carbonyl)phenyl]- 7.43 (m, 2H), 7.36-7.41 (m, 2H), 7.32-7.36 1,3-dihydro-2H- (m, 2H), 6.98 (d, J = 9.1 Hz, 1H), 4.79-4.80 isoindole-2- (bs, 4H), 3.50-3.74 (m, 8H) carboxamide 111 N-{4-[(3,4,5- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) trimethoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.91-9.93 (bs, 1H), 8.33- m/e 446 1,3-dihydro-2H- 8.35 (bs, 1H), 8.17-8.20 (m, 2H), 7.92-7.95 (M − H)⁻ isoindole-2- (m, 2H), 7.43 (s, 2H), 7.20-7.25 (m, 2H), carboxamide 7.15-7.19 (m, 2H), 4.84 (s, 4H), 3.87 (d, J = 0.4 Hz, 3H), 3.74 (s, 6H) 112 N-{4-[(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylpiperidin-1- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 7.90- m/e 364 yl)carbonyl]phenyl}- 7.92 (m, 2H), 7.51-7.54 (m, 2H), 7.19-7.25 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 4.21-4.27 (m, 2H), 2.82 (ddd, J = 13.2, 12.1, carboxamide 2.7 Hz, 2H), 1.44-1.50 (m, 3H), 1.01-1.12 (m, 2H), 0.83 (d, J = 6.1 Hz, 3H) 113 N-[4-({2-[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (APCI(+)) (dimethylamino)phe- Oxide) δ ppm 7.73-7.76 (m, 2H), 7.64-7.66 m/e 429 nyl]ethyl}carbamoyl)phenyl]- (m, 2H), 7.36-7.41 (m, 2H), 7.30-7.36 (m, (M + H)⁺ 1,3-dihydro- 4H), 7.21-7.25 (m, 2H), 4.78-4.80 (bs, 4H), 2H-isoindole-2- 3.47 (t, J = 7.3 Hz, 2H), 3.05 (s, 6H), 2.83- carboxamide 2.88 (m, 2H) 114 N-(4-{[3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (trifluoromethoxy)ben- Oxide) δ ppm 9.03 (t, J = 6.0 Hz, 1H), 8.67- m/e 456 zyl]carbamoyl}phenyl)- 8.69 (bs, 1H), 7.81-7.83 (m, 2H), 7.67-7.69 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.48 (t, J = 7.9 Hz, 1H), 7.36-7.41 isoindole-2- (m, 2H), 7.34-7.37 (m, 1H), 7.31-7.35 (m, carboxamide 2H), 7.28-7.29 (bs, 1H), 7.24 (dd, J = 8.2, 2.2 Hz, 1H), 4.79-4.80 (bs, 4H), 4.51 (d, J = 5.6 Hz, 2H) 115 N-(4-{[(1R)-3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) hydroxy-1- Temp = 90° C.) δ ppm 8.45-8.49 (m, 1H), 8.28- m/e 414 phenylpropyl]carbamoyl}phenyl)- 8.29 (bs, 1H), 8.08-8.12 (m, 2H), 7.87-7.90 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.55-7.59 (m, 2H), 7.26-7.33 (m, isoindole-2- 2H), 7.19-7.23 (m, 3H), 7.16-7.18 (m, 2H), carboxamide 5.79 (td, J = 7.9, 5.4 Hz, 1H), 4.82 (s, 4H), 3.88-3.99 (m, 2H), 2.19-2.43 (m, 2H) 116 N-{4-[(3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) cyanophenyl)carbamoyl]phenyl}- Oxide) δ ppm 8.23 (t, J = 1.8 Hz, 1H), 8.04 m/e 381 1,3-dihydro-2H- (ddd, J = 8.0, 2.3, 1.5 Hz, 1H), 7.91-7.94 (m, (M − H)⁻ isoindole-2- 2H), 7.71-7.78 (m, 2H), 7.59 (t, J = 7.9 Hz, carboxamide 1H), 7.56 (dt, J = 7.6, 1.5 Hz, 1H), 7.38-7.41 (m, 2H), 7.33-7.36 (m, 2H), 4.75-4.87 (m, 4H) 117 N-{4-[(3-fluoro-4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) methoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 10.07-10.09 (bs, 1H), m/e 404 1,3-dihydro-2H- 8.33-8.34 (bs, 1H), 8.13-8.16 (m, 2H), 8.01 (M − H)⁻ isoindole-2- (dd, J = 13.5, 2.5 Hz, 1H), 7.91-7.93 (m, carboxamide 2H), 7.57-7.60 (m, 1H), 7.20-7.23 (m, 2H), 7.15-7.19 (m, 2H), 6.98 (t, J = 9.1 Hz, 1H), 4.84 (s, 4H), 3.73 (s, 3H) 118 N-{4-[(2,3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.11-9.13 (bs, 1H), 8.40- m/e 418 1,3-dihydro-2H- 8.44 (m, 1H), 8.37 (dd, J = 8.4, 1.3 Hz, 1H), (M + H)⁺ isoindole-2- 8.08-8.11 (m, 2H), 7.96-7.99 (m, 2H), 7.21- carboxamide 7.23 (m, 2H), 7.17-7.19 (m, 2H), 7.06 (t, J = 8.3 Hz, 1H), 6.74 (dd, J = 8.3, 1.3 Hz, 1H), 4.85 (s, 4H), 3.88 (s, 3H), 3.74 (s, 3H) 119 N-(4-{[2-(2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) fluorophenyl)ethyl]carbamoyl}phenyl)- Oxide) δ ppm 8.64-8.65 (bs, 1H), 8.48 (t, J = m/e 402 1,3-dihydro-2H- 5.7 Hz, 1H), 7.72-7.74 (m, 2H), 7.62-7.66 (M − H)⁻ isoindole-2- (m, 2H), 7.36-7.42 (m, 2H), 7.31-7.36 (m, carboxamide 2H), 7.25-7.32 (m, 2H), 7.12-7.17 (m, 2H), 4.79-4.88 (m, 4H), 3.47-3.51 (m, 2H), 2.89 (t, J = 7.2 Hz, 2H) 120 N-[4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) (isobutylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.27-8.29 (bs, 1H), 8.09- m/e 338 1,3-dihydro- 8.12 (m, 2H), 7.90-7.93 (m, 2H), 7.84-7.90 (M + H)⁺ 2H-isoindole-2- (m, 1H), 7.19-7.23 (m, 2H), 7.14-7.19 (m, carboxamide 2H), 4.84 (s, 4H), 3.39 (dd, J = 6.8, 6.0 Hz, 2H), 1.91-2.03 (m, 1H), 0.93 (d, J = 6.7 Hz, 6H) 121 N-(4-{[2-(1,3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) benzodioxol-5- Oxide) δ ppm 8.64-8.66 (bs, 1H), 8.42 (t, J = m/e 430 yl)ethyl]carbamoyl}phenyl)- 5.6 Hz, 1H), 7.73-7.75 (m, 2H), 7.63-7.67 (M + H)⁺ 1,3-dihydro- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.36 (m, 2H-isoindole-2- 2H), 6.81-6.84 (m, 2H), 6.71 (dd, J = 7.8, 1.7 carboxamide Hz, 1H), 5.95 (s, 2H), 4.78-4.79 (bs, 4H), 3.41-3.46 (m, 2H), 2.73-2.78 (m, 2H) 122 N-(4-{[2-(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyphenyl)eth- Temp = 90° C.) δ ppm 8.25-8.27 (bs, 1H), 8.05- m/e 416 yl]carbamoyl}phenyl)- 8.08 (m, 2H), 7.98-8.02 (bs, 1H), 7.89-7.92 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.19-7.25 (m, 3H), 7.14-7.19 (m, isoindole-2- 3H), 6.83-6.90 (m, 2H), 4.84 (s, 4H), 3.83- carboxamide 3.88 (m, 2H), 3.66 (s, 3H), 3.09 (t, J = 7.1 Hz, 2H) 123 N-[4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) (butylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.27-8.28 (bs, 1H), 8.09- m/e 338 1,3-dihydro-2H- 8.12 (m, 2H), 7.89-7.93 (m, 2H), 7.86-7.92 (M + H)⁺ isoindole-2- (m, 1H), 7.19-7.23 (m, 2H), 7.15-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 3.48-3.61 (m, 2H), 1.62 (p, J = 7.2 Hz, 2H), 1.26-1.44 (m, 2H), 0.85 (t, J = 7.3 Hz, 3H) 124 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) isopropoxyethyl)carbamoyl]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.75-7.78 (m, m/e 366 1,3-dihydro-2H- 2H), 7.63-7.66 (m, 2H), 7.26-7.40 (m, 4H), (M − H)⁻ isoindole-2- 4.82 (s, 4H), 3.58-3.68 (m, 1H), 3.52-3.56 carboxamide (m, 2H), 3.42 (t, J = 6.2 Hz, 2H), 1.12 (d, J = 6.1 Hz, 6H) 125 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) isopropoxypropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.28-8.30 (bs, 1H), 8.07- m/e 382 1,3-dihydro-2H- 8.10 (m, 2H), 7.93-7.97 (m, 1H), 7.90-7.94 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.14-7.19 (m, carboxamide 2H), 4.85 (s, 4H), 3.62-3.74 (m, 2H), 3.42- 3.55 (m, 3H), 1.92 (p, J = 6.4 Hz, 2H), 1.08 (d, J = 6.1 Hz, 6H) 126 4-chloro-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.66 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 8.29 (t, J = 5.6 Hz, 1H), 7.75-7.79 m/e 434 1,3-dihydro-2H- (m, 2H), 7.64-7.68 (m, 2H), 7.33-7.41 (m, (M + H)⁺ isoindole-2- 3H), 7.13-7.32 (m, 5H), 4.77-4.89 (m, 4H), carboxamide 3.19-3.31 (m, 2H), 2.58-2.68 (m, 2H), 1.76- 1.89 (m, 2H) 127 N-(4-{[2-(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) methoxyphenyl)eth- Oxide) δ ppm 8.64-8.66 (bs, 1H), 8.43 (t, J = m/e 416 yl]carbamoyl}phenyl)- 5.6 Hz, 1H), 7.73-7.76 (m, 2H), 7.63-7.65 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.35 (m, isoindole-2- 2H), 7.16-7.19 (m, 2H), 6.86-6.88 (m, 2H), carboxamide 4.78-4.80 (bs, 4H), 3.72 (s, 3H), 3.42-3.51 (m, 2H), 2.78 (t, J = 7.4 Hz, 2H) 128 N-{4-[(3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) methoxypropyl)carbamoyl]phenyl}- Oxide) δ ppm 7.75-7.78 (m, 2H), 7.60-7.69 m/e 354 1,3-dihydro-2H- (m, 2H), 7.37-7.40 (m, 2H), 7.32-7.35 (m, (M + H)⁺ isoindole-2- 2H), 4.79-4.80 (bs, 4H), 3.39 (t, J = 6.3 Hz, carboxamide 2H), 3.30 (t, J = 7.0 Hz, 2H), 3.25 (s, 3H), 1.76 (p, J = 6.7 Hz, 2H) 129 N-(4-{[2-(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) fluorophenyl)ethyl]carbamoyl}phenyl)- Oxide) δ ppm 8.64-8.66 (bs, 1H), 8.45 (t, J = m/e 404 1,3-dihydro-2H- 5.6 Hz, 1H), 7.73-7.75 (m, 2H), 7.63-7.66 (M + H)⁺ isoindole-2- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.35 (m, carboxamide 2H), 7.27-7.31 (m, 2H), 7.09-7.13 (m, 2H), 4.78-4.80 (bs, 4H), 3.47 (t, J = 7.3 Hz, 2H), 2.84 (t, J = 7.3 Hz, 2H) 130 N-(4-{[3-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) oxopyrrolidin-1- (s, 1H), 8.27 (t, J = 5.7 Hz, 1H), 7.74-7.78 m/e 407 yl)propyl]carbamoyl}phenyl)- (m, 2H), 7.64-7.69 (m, 2H), 7.30-7.39 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 4.78-4.79 (bs, 4H), 3.32-3.39 (m, 2H), isoindole-2- 3.17-3.26 (m, 4H), 2.22 (t, J = 8.0 Hz, 2H), carboxamide 1.87-1.97 (m, 2H), 1.69 (p, J = 7.0 Hz, 2H) 131 N-{4-[(2,4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.89-8.91 (bs, 1H), 8.53 m/e 418 1,3-dihydro-2H- (d, J = 8.7 Hz, 1H), 8.36-8.37 (bs, 1H), 8.10- (M + H)⁺ isoindole-2- 8.13 (m, 2H), 7.95-7.98 (m, 2H), 7.19-7.24 carboxamide (m, 2H), 7.15-7.19 (m, 2H), 6.67 (d, J = 2.6 Hz, 1H), 6.61 (dd, J = 8.7, 2.7 Hz, 1H), 4.85 (s, 4H), 3.72 (s, 3H), 3.69 (s, 3H) 133 N-{4-[(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) phenoxyethyl)carbamoyl]phenyl}- (s, 1H), 8.52 (t, J = 5.5 Hz, 1H), 7.77-7.81 m/e 402 1,3-dihydro-2H- (m, 2H), 7.65-7.69 (m, 2H), 7.26-7.39 (m, (M + H)⁺ isoindole-2- 6H), 6.90-6.99 (m, 3H), 4.79 (s, 4H), 4.10 (t, carboxamide J = 5.9 Hz, 2H), 3.62 (q, J = 5.7 Hz, 2H) 134 N-(4-{[2-(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) hydroxyphenyl)eth- Oxide) δ ppm 7.73-7.76 (m, 2H), 7.63-7.66 m/e 402 yl]carbamoyl}phenyl)- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.36 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 7.04-7.07 (m, 2H), 6.69-6.71 (m, 2H), isoindole-2- 4.79-4.80 (bs, 4H), 3.41 (dd, J = 8.5, 6.5 Hz, carboxamide 2H), 2.73 (t, J = 7.5 Hz, 2H) 135 N-(4-{[2-(3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) fluorophenyl)ethyl]carbamoyl}phenyl)- Oxide) δ ppm 8.64-8.66 (bs, 1H), 8.46 (t, J = m/e 404 1,3-dihydro-2H- 5.6 Hz, 1H), 7.72-7.75 (m, 2H), 7.63-7.66 (M + H)⁺ isoindole-2- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.35 (m, carboxamide 3H), 7.08-7.11 (m, 2H), 7.00-7.05 (m, 1H), 4.78-4.79 (bs, 4H), 3.50 (t, J = 6.9 Hz, 2H), 2.88 (t, J = 7.2 Hz, 2H) 136 N-[4-({1-[(3S)- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.25 (ESI(+)) tetrahydrofuran-3- (s, 1H), 8.64 (s, 1H), 8.08 (s, 1H), 7.85-7.89 m/e 418 yl]-1H-pyrazol-4- (m, 2H), 7.70-7.75 (m, 2H), 7.61 (s, 1H), (M + H)⁺ yl}carbamoyl)phenyl]- 7.29-7.41 (m, 4H), 4.94-5.06 (m, 1H), 4.80- 1,3-dihydro-2H- 4.81 (bs, 4H), 3.93-4.01 (m, 2H), 3.78-3.89 isoindole-2- (m, 2H), 2.30-2.46 (m, 1H), 2.14-2.30 (m, 1H) carboxamide 137 5-methyl-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 8.29 (t, J = 5.6 Hz, 1H), 7.74-7.79 m/e 414 1,3-dihydro-2H- (m, 2H), 7.63-7.68 (m, 2H), 7.11-7.34 (m, (M + H)⁺ isoindole-2- 8H), 4.73-4.74 (bs, 4H), 3.20-3.30 (m, 2H), carboxamide 2.63 (t, J = 7.6 Hz, 2H), 2.33 (s, 3H), 1.82 (p, J = 7.4 Hz, 2H) 138 N-[4-(1,4-dioxa-8- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) azaspiro[4.5]dec-8- Temp = 90° C.) δ ppm 8.27-8.28 (bs, 1H), 7.89- m/e 408 ylcarbonyl)phenyl]- 7.92 (m, 2H), 7.52-7.55 (m, 2H), 7.19-7.23 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.16-7.18 (m, 2H), 4.85 (s, 4H), isoindole-2- 3.84 (s, 4H), 3.73-3.76 (m, 4H), 1.71-1.75 carboxamide (m, 4H) 139 N-{4-[(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) phenylethyl)carbamoyl]phenyl}- (s, 1H), 8.38 (t, J = 5.6 Hz, 1H), 7.73-7.77 m/e 386 1,3-dihydro-2H- (m, 2H), 7.64-7.67 (m, 2H), 7.20-7.39 (m, (M + H)⁺ isoindole-2- 9H), 4.79 (s, 4H), 3.43-3.50 (m, 2H), 2.80- carboxamide 2.88 (m, 2H) 140 N-(4-{[2-(2,4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethoxyphenyl)eth- Temp = 90° C.) δ ppm 8.25-8.26 (bs, 1H), 8.07- m/e 446 yl]carbamoyl}phenyl)- 8.09 (m, 2H), 7.95-8.02 (m, 1H), 7.88-7.93 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.19-7.24 (m, 2H), 7.13-7.19 (m, isoindole-2- 2H), 6.57 (d, J = 2.4 Hz, 1H), 6.49 (dd, J = carboxamide 8.1, 2.4 Hz, 1H), 4.84 (s, 4H), 3.81-3.85 (m, 2H), 3.68 (s, 3H), 3.66 (s, 3H), 3.04 (t, J = 7.0 Hz, 2H) 141 N-(4-{[3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (methylthio)propyl]carbamoyl}phenyl)- Oxide, Temp = 90° C.) δ ppm 7.76-7.78 (m, m/e 370 1,3-dihydro-2H- 2H), 7.63-7.65 (m, 2H), 7.32-7.40 (m, 4H), (M + H)⁺ isoindole-2- 4.82 (s, 4H), 3.37 (t, J = 6.9 Hz, 2H), 2.53- carboxamide 2.57 (m, 2H), 2.09 (s, 3H), 1.85 (p, J = 7.1 Hz, 2H) 142 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) ethoxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.28-8.34 (m, 1H), 8.07- m/e 354 1,3-dihydro-2H- 8.12 (m, 2H), 8.01-8.08 (m, 1H), 7.89-7.92 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.24 (m, 2H), 7.14-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 3.76 (q, J = 5.7 Hz, 2H), 3.63 (t, J = 5.7 Hz, 2H), 3.43 (q, J = 6.9 Hz, 2H), 1.09 (t, J = 6.9 Hz, 3H) 143 N-{4-[(2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) fluorophenyl)carbamoyl]phenyl}- Oxide) δ ppm 7.91-7.93 (m, 2H), 7.72-7.75 m/e 374 1,3-dihydro-2H- (m, 2H), 7.56-7.65 (m, 1H), 7.37-7.42 (m, (M − H)⁻ isoindole-2- 2H), 7.32-7.37 (m, 2H), 7.26-7.31 (m, 2H), carboxamide 7.21-7.26 (m, 1H), 4.78-4.82 (m, 4H) 144 N-(4-{[2-(pyridin-3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) yl)ethyl]carbamoyl}phenyl)- (s, 1H), 8.45 (d, J = 2.2 Hz, 1H), 8.41 (dd, J = m/e 387 1,3-dihydro- 4.7, 1.6 Hz, 1H), 8.38 (d, J = 5.5 Hz, 1H), (M + H)⁺ 2H-isoindole-2- 7.71-7.75 (m, 2H), 7.63-7.68 (m, 3H), 7.29- carboxamide 7.39 (m, 5H), 4.79 (s, 4H), 3.46-3.53 (m, 2H), 2.87 (t, J = 7.1 Hz, 2H) 145 N-[4-({4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) [(trifluoromethyl)thio]ben- Oxide) δ ppm 9.03 (t, J = 6.0 Hz, 1H), 8.67- m/e 472 zyl}carbamoyl)phenyl]- 8.70 (bs, 1H), 7.82-7.84 (m, 2H), 7.66-7.70 (M + H)⁺ 1,3-dihydro- (m, 4H), 7.47-7.49 (m, 2H), 7.36-7.41 (m, 2H-isoindole-2- 2H), 7.31-7.36 (m, 2H), 4.79-4.80 (bs, 4H), carboxamide 4.53 (d, J = 5.3 Hz, 2H) 146 N-{4-[(3,4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.90-9.92 (bs, 1H), 8.32- m/e 418 1,3-dihydro-2H- 8.33 (bs, 1H), 8.17-8.19 (m, 2H), 7.92-7.94 (M + H)⁺ isoindole-2- (m, 2H), 7.77 (d, J = 2.4 Hz, 1H), 7.49-7.53 carboxamide (m, 1H), 7.20-7.23 (m, 2H), 7.14-7.19 (m, 2H), 6.94 (d, J = 8.6 Hz, 1H), 4.84 (s, 4H), 3.74 (s, 6H) 147 N-(4-{[3-(2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) fluorophenyl)pyrrolidin-1- Oxide) δ ppm 7.60-7.67 (m, 2H), 7.47-7.55 m/e 430 yl]carbonyl}phenyl)- (m, 2H), 7.26-7.45 (m, 6H), 7.12-7.25 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 4.77-4.82 (m, 4H), 3.83-3.97 (m, 1H), isoindole-2- 3.47-3.64 (m, 4H), 2.19-2.36 (m, 1H), 1.98- carboxamide 2.18 (m, 1H) 148 N-(4-{[3-(1H- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) imidazol-1- Temp = 90° C.) δ ppm 8.36-8.38 (bs, 1H), 8.24- m/e 390 yl)propyl]carbamoyl}phenyl)- 8.31 (m, 1H), 8.08-8.12 (m, 2H), 8.00-8.05 (M + H)⁺ 1,3-dihydro-2H- (bs, 1H), 7.91-7.97 (m, 2H), 7.25-7.31 (bs, isoindole-2- 1H), 7.19-7.24 (m, 2H), 7.16-7.19 (m, 2H), carboxamide 4.86 (s, 4H), 4.06 (t, J = 7.0 Hz, 2H), 3.55 (q, J = 6.4 Hz, 2H), 2.11 (p, J = 6.9 Hz, 2H) 149 N-(4-{[2-(3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (APCI(+)) chlorophenyl)ethyl]carbamoyl}phenyl)- Oxide) δ ppm 8.64-8.66 (bs, 1H), 8.45 (t, J = m/e 420 1,3-dihydro-2H- 5.6 Hz, 1H), 7.72-7.75 (m, 2H), 7.63-7.66 (M + H)⁺ isoindole-2- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.36 (m, carboxamide 4H), 7.25-7.29 (m, 1H), 7.21-7.24 (m, 1H), 4.76-4.81 (bs, 4H), 3.47-3.51 (m, 2H), 2.86 (t, J = 7.2 Hz, 2H) 150 N-{4-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) hydroxybutyl)carbamoyl]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.75-7.78 (m, m/e 354 1,3-dihydro-2H- 2H), 7.62-7.65 (m, 2H), 7.32-7.40 (m, 4H), (M + H)⁺ isoindole-2- 4.81 (s, 4H), 3.48 (t, J = 6.3 Hz, 2H), 3.28- carboxamide 3.32 (m, 2H), 1.49-1.65 (m, 4H) 151 N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 8.30 (t, J = 5.6 Hz, 1H), 7.74-7.81 m/e 468 5-(trifluoromethyl)-1,3- (m, 3H), 7.57-7.73 (m, 4H), 7.15-7.32 (m, (M + H)⁺ dihydro-2H- 5H), 4.85-4.87 (bs, 4H), 3.27 (q, J = 6.6 Hz, isoindole-2- 2H), 2.63 (t, J = 7.6 Hz, 2H), 1.83 (p, J = 7.4 carboxamide Hz, 2H) 152 N-(4-{[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (APCI(+)) (hydroxymethyl)phe- Oxide) δ ppm 7.90-7.92 (m, 2H), 7.68-7.74 m/e 388 nyl]carbamoyl}phenyl)- (m, 4H), 7.38-7.41 (m, 2H), 7.33-7.36 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 7.29-7.32 (m, 2H), 4.78-4.84 (m, 4H), isoindole-2- 4.47 (s, 2H) carboxamide 153 N-[4-(1,3- ¹H NMR (400 MHz, Pyridine-d₅, (APCI(+)) benzodioxol-5- Temp = 90° C.) δ ppm 9.95-9.97 (bs, 1H), 8.28- m/e 402 ylcarbamoyl)phenyl]- 8.36 (m, 1H), 8.13-8.15 (m, 2H), 7.90-7.93 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.76 (d, J = 2.1 Hz, 1H), 7.32 (dd, J = isoindole-2- 8.3, 2.1 Hz, 1H), 7.19-7.23 (m, 2H), 7.15- carboxamide 7.19 (m, 2H), 6.82 (d, J = 8.3 Hz, 1H), 5.86 (s, 2H), 4.84 (s, 4H) 154 N-{4-[(1-isopropyl- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.21 (ESI(+)) 1H-pyrazol-4- (s, 1H), 8.64 (s, 1H), 8.03 (d, J = 0.7 Hz, m/e 390 yl)carbamoyl]phenyl}- 1H), 7.85-7.89 (m, 2H), 7.70-7.74 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.57 (d, J = 0.7 Hz, 1H), 7.30-7.40 (m, 4H), isoindole-2- 4.80-4.81 (bs, 4H), 4.41-4.55 (m, 1H), 1.41 carboxamide (d, J = 6.7 Hz, 6H) 155 N-{4-[(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.83-9.85 (bs, 1H), 8.29- m/e 374 1,3-dihydro-2H- 8.33 (bs, 1H), 8.16-8.18 (m, 2H), 7.91-7.93 (M + H)⁺ isoindole-2- (m, 2H), 7.86-7.89 (m, 2H), 7.19-7.23 (m, carboxamide 2H), 7.17-7.19 (m, 3H), 7.10-7.12 (m, 2H), 4.84 (s, 4H) 156 N-{4-[(1-ethyl-1H- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.22 (ESI(+)) pyrazol-4- (s, 1H), 8.64 (s, 1H), 8.03 (s, 1H), 7.85-7.90 m/e 376 yl)carbamoyl]phenyl}- (m, 2H), 7.70-7.74 (m, 2H), 7.57 (s, 1H), (M + H)⁺ 1,3-dihydro-2H- 7.30-7.40 (m, 4H), 4.80-4.81 (bs, 4H), 4.11 isoindole-2- (q, J = 7.2 Hz, 2H), 1.36 (t, J = 7.2 Hz, 3H) carboxamide 157 N-{4-[(2,5- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.97-8.99 (bs, 1H), 8.56 m/e 418 1,3-dihydro-2H- (d, J = 3.0 Hz, 1H), 8.40-8.42 (bs, 1H), 8.07- (M + H)⁺ isoindole-2- 8.10 (m, 2H), 7.96-7.98 (m, 2H), 7.21-7.24 carboxamide (m, 2H), 7.16-7.19 (m, 2H), 6.88 (d, J = 8.8 Hz, 1H), 6.69 (dd, J = 8.8, 3.0 Hz, 1H), 4.85 (s, 4H), 3.72 (s, 3H), 3.71 (s, 3H) 158 N-{4-[methyl(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.51 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 7.60-7.64 (m, 2H), 7.11-7.44 (m, m/e 414 1,3-dihydro-2H- 11H), 4.78-4.79 (bs, 4H), 3.26-3.52 (m, 2H), (M + H)⁺ isoindole-2- 2.94 (s, 3H), 2.34-2.70 (m, 2H), 1.82-1.91 carboxamide (m, 2H) 159 N-{4-[(2-hydroxy-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) methylpropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.30-8.32 (bs, 1H), 8.06- m/e 352 1,3-dihydro-2H- 8.09 (m, 2H), 7.89-7.95 (m, 1H), 7.89-7.92 (M − H)⁻ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.15-7.19 (m, carboxamide 2H), 4.84 (s, 4H), 3.70 (d, J = 5.9 Hz, 2H), 1.38 (s, 6H) 160 N-(4-{[4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) (trifluoromethyl)piperidin-1- Temp = 90° C.) δ ppm 8.31-8.33 (bs, 1H), 7.91- m/e 416 yl]carbonyl}phenyl)- 7.94 (m, 2H), 7.50-7.55 (m, 2H), 7.19-7.24 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.86 (s, 4H), isoindole-2- 4.34-4.39 (m, 2H), 2.83 (td, J = 12.9, 2.8 Hz, carboxamide 2H), 2.24-2.43 (m, 1H), 1.73-1.77 (m, 2H), 1.50 (qd, J = 12.5, 4.4 Hz, 2H) 161 N-[4-(thiomorpholin- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) 4-ylcarbonyl)phenyl]- Temp = 90° C.) δ ppm 8.29-8.31 (bs, 1H), 7.90- m/e 368 1,3-dihydro-2H- 7.92 (m, 2H), 7.47-7.50 (m, 2H), 7.20-7.23 (M + H)⁺ isoindole-2- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), carboxamide 3.81-3.84 (m, 4H), 2.54-2.58 (m, 4H) 162 N-[4-(5,6- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) dihydroimidazo[1,5- (s, 1H), 7.67-7.71 (m, 2H), 7.60-7.62 (bs, m/e 388 a]pyrazin-7(8H)- 1H), 7.30-7.43 (m, 6H), 6.72-6.77 (bs, 1H), (M + H)⁺ ylcarbonyl)phenyl]- 4.79-4.80 (bs, 4H), 4.73-4.75 (bs, 2H), 4.06- 1,3-dihydro-2H- 4.18 (m, 2H), 3.81-3.88 (m, 2H) isoindole-2- carboxamide 163 N-(4-{[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) furoyl)piperazin-1- Temp = 90° C.) δ ppm 8.31-8.34 (m, 1H), 7.92- m/e 443 yl]carbonyl}phenyl)- 7.95 (m, 2H), 7.57-7.59 (m, 1H), 7.53-7.57 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.20-7.24 (m, 2H), 7.16-7.19 (m, isoindole-2- 2H), 7.08-7.09 (m, 1H), 6.45 (dd, J = 3.4, 1.7 carboxamide Hz, 1H), 4.86 (s, 4H), 3.75-3.80 (m, 4H), 3.64-3.70 (m, 4H) 164 N-{4-[(1- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) benzylpiperidin-4- Oxide, Temp = 90° C.) δ ppm 7.77-7.80 (m, m/e 455 yl)carbamoyl]phenyl}- 2H), 7.65-7.67 (m, 2H), 7.49-7.56 (m, 5H), (M + H)⁺ 1,3-dihydro-2H- 7.37-7.43 (m, 2H), 7.32-7.36 (m, 2H), 4.82 isoindole-2- (s, 4H), 4.31-4.32 (bs, 2H), 4.03-4.10 (m, carboxamide 1H), 3.39-3.44 (m, 2H), 3.12-3.19 (m, 2H), 2.08-2.14 (m, 2H), 1.88-1.99 (m, 2H) 165 N-{4-[(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.91-9.93 (bs, 1H), 8.33- m/e 388 1,3-dihydro-2H- 8.34 (bs, 1H), 8.16-8.18 (m, 2H), 7.86-7.98 (M + H)⁺ isoindole-2- (m, 4H), 7.20-7.23 (m, 2H), 7.15-7.19 (m, carboxamide 2H), 6.95-6.98 (m, 2H), 4.85 (s, 4H), 3.67 (s, 3H) 166 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.99-10.01 (m, 1H), m/e 388 1,3-dihydro-2H- 8.34-8.35 (bs, 1H), 8.10-8.20 (m, 2H), 7.91- (M + H)⁺ isoindole-2- 7.94 (m, 2H), 7.82 (t, J = 2.2 Hz, 1H), 7.57- carboxamide 7.60 (m, 1H), 7.21-7.24 (m, 2H), 7.14-7.19 (m, 2H), 6.75 (dd, J = 8.2, 2.5 Hz, 1H), 4.84 (s, 4H), 3.68 (s, 3H) 167 N-{4-[(5-acetamido-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.89-9.92 (bs, 1H), 8.93- m/e 445 1,3-dihydro-2H- 8.97 (m, 2H), 8.38-8.39 (bs, 1H), 8.04-8.07 (M + H)⁺ isoindole-2- (m, 2H), 7.93-7.96 (m, 2H), 7.87-7.93 (m, carboxamide 1H), 7.20-7.25 (m, 2H), 7.15-7.19 (m, 2H), 6.91 (d, J = 8.8 Hz, 1H), 4.85 (s, 4H), 3.71 (d, J = 1.1 Hz, 3H), 2.14 (d, J = 0.9 Hz, 3H) 168 N-(4-{[2-(3,5- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) dimethoxyphenyl)eth- Temp = 90° C.) δ ppm 8.25-8.28 (bs, 1H), 8.08- m/e 444 yl]carbamoyl}phenyl)- 8.13 (m, 1H), 8.07-8.11 (m, 2H), 7.87-7.92 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.19-7.24 (m, 2H), 7.14-7.19 (m, isoindole-2- 2H), 6.56-6.59 (m, 2H), 6.47-6.50 (m, 1H), carboxamide 4.84 (s, 4H), 3.82-3.88 (m, 2H), 3.65 (s, 6H), 3.00 (t, J = 7.2 Hz, 2H) 169 N-[4-({2-[3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (trifluoromethyl)phe- Oxide) δ ppm 8.63-8.66 (bs, 1H), 8.45 (t, J = m/e 454 nyl]ethyl}carbamoyl)phenyl]- 5.6 Hz, 1H), 7.70-7.73 (m, 2H), 7.62-7.65 (M + H)⁺ 1,3-dihydro- (m, 2H), 7.53-7.61 (m, 4H), 7.37-7.40 (m, 2H-isoindole-2- 2H), 7.32-7.35 (m, 2H), 4.78-4.79 (bs, 4H), carboxamide 3.50-3.56 (m, 2H), 2.96 (t, J = 7.1 Hz, 2H) 170 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylbutan-2- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 7.96- m/e 352 yl)carbamoyl]phenyl}- 7.99 (m, 2H), 7.86-7.88 (m, 2H), 7.18-7.24 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.14-7.19 (m, 2H), 6.76-6.79 (bs, isoindole-2- 1H), 4.83 (s, 4H), 1.94 (q, J = 7.5 Hz, 2H), carboxamide 1.47 (s, 6H), 0.90 (t, J = 7.4 Hz, 3H) 171 N-(4-{[2-(1H- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) imidazol-4- Temp = 90° C.) δ ppm 8.48-8.52 (bs, 1H), 8.32- m/e 376 yl)ethyl]carbamoyl}phenyl)- 8.34 (bs, 1H), 8.27 (s, 1H), 8.09-8.12 (m, (M + H)⁺ 1,3-dihydro- 2H), 7.90-7.93 (m, 2H), 7.19-7.23 (m, 2H), 2H-isoindole-2- 7.16-7.19 (m, 2H), 4.84 (s, 4H), 3.90-3.96 carboxamide (m, 2H), 3.13 (t, J = 6.7 Hz, 2H) 172 N-(4-{[(2S)-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) hydroxypropyl]carbamoyl}phenyl)- Temp = 90° C.) δ ppm 8.28-8.30 (bs, 1H), 8.06- m/e 338 1,3-dihydro-2H- 8.10 (m, 2H), 8.03-8.09 (m, 1H), 7.88-7.91 (M − H)⁻ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.15-7.19 (m, carboxamide 2H), 4.84 (s, 4H), 4.25 (dddd, J = 12.4, 7.0, 6.3, 4.2 Hz, 1H), 3.78 (ddd, J = 13.4, 6.1, 4.3 Hz, 1H), 3.61 (ddd, J = 13.4, 6.9, 5.4 Hz, 1H), 1.31 (d, J = 6.2 Hz, 3H) 173 N-(4-{[(1R)-1-(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) cyanophenyl)ethyl]carbamoyl}phenyl)- Temp = 90° C.) δ ppm 8.32-8.37 (m, 1H), 8.28- m/e 411 1,3-dihydro-2H- 8.32 (bs, 1H), 8.09-8.12 (m, 2H), 7.88-7.90 (M + H)⁺ isoindole-2- (m, 2H), 7.83 (s, 1H), 7.69-7.72 (m, 1H), carboxamide 7.43-7.47 (m, 1H), 7.30 (t, J = 7.8 Hz, 1H), 7.19-7.24 (m, 2H), 7.14-7.18 (m, 2H), 5.55 (p, J = 7.1 Hz, 1H), 4.83 (s, 4H), 1.56 (d, J = 7.0 Hz, 3H) 174 N-(4-{[(2S)-1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxy-3- Temp = 90° C.) δ ppm 8.29-8.31 (bs, 1H), 8.05- m/e 366 methylbutan-2- 8.08 (m, 2H), 7.87-7.90 (m, 2H), 7.46-7.53 (M + H)⁺ yl]carbamoyl}phenyl)- (bs, 1H), 7.19-7.24 (m, 2H), 7.14-7.18 (m, 1,3-dihydro-2H- 2H), 4.84 (s, 4H), 4.29-4.36 (m, 1H), 3.99 (d, isoindole-2- J = 4.8 Hz, 2H), 2.17-2.28 (m, 1H), 1.00- carboxamide 1.10 (m, 6H) 175 N-{4-[benzyl(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) hydroxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.20-8.21 (bs, 1H), 7.85- m/e 414 1,3-dihydro-2H- 7.88 (m, 2H), 7.61-7.64 (m, 2H), 7.37-7.43 (M − H)⁻ isoindole-2- (m, 2H), 7.29-7.34 (m, 2H), 7.20-7.27 (m, carboxamide 3H), 7.14-7.19 (m, 2H), 4.94-4.94 (bs, 2H), 4.84 (s, 4H), 3.94-3.97 (m, 2H), 3.73 (t, J = 6.0 Hz, 2H) 176 N-{4-[(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) cyanophenyl)carbamoyl]phenyl}- Oxide) δ ppm 7.97-7.99 (m, 2H), 7.91-7.93 m/e 381 1,3-dihydro-2H- (m, 2H), 7.80-7.83 (m, 2H), 7.72-7.77 (m, (M − H)⁻ isoindole-2- 2H), 7.38-7.41 (m, 2H), 7.33-7.36 (m, 2H), carboxamide 4.81 (s, 4H) 177 N-(4-{[2-(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) chlorophenyl)ethyl]carbamoyl}phenyl)- Oxide) δ ppm 8.66 (s, 1H), 8.45 (t, J = 5.6 m/e 420 1,3-dihydro-2H- Hz, 1H), 7.72-7.74 (m, 2H), 7.64 (dd, J = (M + H)⁺ isoindole-2- 8.7, 2.3 Hz, 2H), 7.37-7.40 (m, 2H), 7.32- carboxamide 7.36 (m, 4H), 7.27-7.30 (m, 2H), 4.78-4.79 (bs, 4H), 3.45-3.50 (m, 2H), 2.84 (t, J = 7.2 Hz, 2H) 178 N-(4-{[2-(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylpiperazin-1- Temp = 90° C.) δ ppm 8.34-8.35 (bs, 1H), 8.08- m/e 408 yl)ethyl]carbamoyl}phenyl)- 8.12 (m, 2H), 8.06-8.10 (m, 1H), 7.92-7.94 (M + H)⁺ 1,3-dihydro- (m, 2H), 7.19-7.23 (m, 2H), 7.17-7.19 (m, 2H-isoindole-2- 2H), 4.85 (s, 4H), 3.71 (q, J = 5.9 Hz, 2H), carboxamide 2.85-2.90 (m, 4H), 2.81-2.85 (m, 4H), 2.76 (t, J = 6.3 Hz, 2H), 2.48 (s, 3H) 179 N-(4-{[2-(pyridin-2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) yl)ethyl]carbamoyl}phenyl)- Oxide) δ ppm 8.77 (dd, J = 5.8, 1.6 Hz, 1H), m/e 387 1,3-dihydro- 8.45 (td, J = 7.8, 1.6 Hz, 1H), 7.92 (d, J = 8.0 (M + H)⁺ 2H-isoindole-2- Hz, 1H), 7.88 (ddd, J = 7.5, 6.0, 1.3 Hz, 1H), carboxamide 7.66-7.69 (m, 2H), 7.62-7.65 (m, 2H), 7.36- 7.39 (m, 2H), 7.32-7.35 (m, 2H), 4.78-4.79 (bs, 4H), 3.68-3.72 (m, 2H), 3.25 (t, J = 6.4 Hz, 2H) 180 N-{4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (APCI(+)) [(cyanomethyl)carbamoyl]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.79-7.81 (m, m/e 321 1,3-dihydro-2H- 2H), 7.68-7.71 (m, 2H), 7.36-7.41 (m, 2H), (M + H)⁺ isoindole-2- 7.31-7.36 (m, 2H), 4.82 (s, 4H), 4.28 (s, 2H) carboxamide 181 N-[4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) (cyclohexylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 8.05- m/e 364 1,3-dihydro-2H- 8.08 (m, 2H), 7.88-7.90 (m, 2H), 7.40-7.47 (M + H)⁺ isoindole-2- (m, 1H), 7.19-7.24 (m, 2H), 7.14-7.19 (m, carboxamide 2H), 4.84 (s, 4H), 4.13-4.20 (m, 1H), 2.05- 2.08 (m, 2H), 1.63-1.67 (m, 2H), 1.47-1.54 (m, 1H), 1.28-1.41 (m, 4H), 1.04-1.17 (m, 1H) 182 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxyphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.93-9.94 (m, 1H), 8.30- m/e 374 1,3-dihydro-2H- 8.32 (m, 1H), 8.10-8.14 (m, 2H), 8.01 (t, J = (M + H)⁺ isoindole-2- 2.2 Hz, 1H), 7.87-7.92 (m, 2H), 7.48 (ddd, J = carboxamide 8.0, 2.0, 0.9 Hz, 1H), 7.25 (t, J = 8.0 Hz, 1H), 7.19-7.25 (m, 2H), 7.13-7.18 (m, 2H), 6.90 (ddd, J = 8.0, 2.4, 1.0 Hz, 1H), 4.83 (s, 4H) 183 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) [butyl(methyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.24-8.26 (bs, 1H), 7.89- m/e 350 1,3-dihydro-2H- 7.92 (m, 2H), 7.49-7.52 (m, 2H), 7.19-7.24 (M + H)⁺ isoindole-2- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), carboxamide 3.41 (t, J = 7.3 Hz, 2H), 2.95 (s, 3H), 1.52 (p, J = 7.3 Hz, 2H), 1.15-1.33 (m, 2H), 0.82 (t, J = 7.3 Hz, 3H) 184 N-(4-{[4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) (dimethylamino)phe- Temp = 90° C.) δ ppm 9.76-9.77 (bs, 1H), 8.30- m/e 399 nyl]carbamoyl}phenyl)- 8.32 (bs, 1H), 8.16-8.19 (m, 2H), 7.91-7.95 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.84-7.86 (m, 2H), 7.20-7.23 (m, isoindole-2- 2H), 7.15-7.19 (m, 2H), 6.73-6.81 (m, 2H), carboxamide 4.85 (s, 4H), 2.77 (s, 6H) 185 N-[4-(3,4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dihydroisoquinolin- Temp = 90° C.) δ ppm 8.29-8.30 (bs, 1H), 7.91- m/e 398 2(1H)- 7.94 (m, 2H), 7.54-7.60 (m, 2H), 7.19-7.26 (M + H)⁺ ylcarbonyl)phenyl]- (m, 2H), 7.15-7.19 (m, 2H), 7.11-7.15 (m, 1,3-dihydro-2H- 2H), 7.05-7.11 (m, 1H), 6.98-7.04 (m, 1H), isoindole-2- 4.86 (s, 4H), 4.80-4.81 (bs, 2H), 3.75 (t, J = carboxamide 5.9 Hz, 2H), 2.78 (t, J = 6.0 Hz, 2H) 186 N-[4-(1,3-dihydro- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) 2H-isoindol-2- Temp = 90° C.) δ ppm 8.34-8.36 (bs, 1H), 7.96- m/e 384 ylcarbonyl)phenyl]- 7.98 (m, 2H), 7.72-7.75 (m, 2H), 7.20-7.24 (M + H)⁺ 1,3-dihydro-2H- (m, 4H), 7.16-7.20 (m, 4H), 4.87-4.90 (bs, isoindole-2- 4H), 4.88 (s, 4H) carboxamide 187 N-[4-(2,3-dihydro- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) 1H-indol-1- Temp = 90° C.) δ ppm 8.36-8.38 (m, 1H), 7.96- m/e 384 ylcarbonyl)phenyl]- 8.00 (m, 1H), 7.93-7.97 (m, 2H), 7.63-7.65 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.20-7.24 (m, 2H), 7.15-7.20 (m, isoindole-2- 2H), 7.11-7.15 (m, 2H), 6.96-7.00 (m, 1H), carboxamide 4.87 (s, 4H), 3.94-3.99 (m, 2H), 2.89 (t, J = 8.3 Hz, 2H) 188 N-[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) (phenylcarbamoyl)phenyl]- Oxide) δ ppm 7.90-7.92 (m, 2H), 7.72-7.77 m/e 356 1,3-dihydro- (m, 4H), 7.33-7.40 (m, 6H), 7.12 (t, J = 7.3 (M − H)⁻ 2H-isoindole-2- Hz, 1H), 4.80-4.82 (bs, 4H) carboxamide 189 N-{4-[(4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) fluorophenyl)carbamoyl]phenyl}- Oxide) δ ppm 10.17-10.19 (bs, 1H), 8.72- m/e 376 1,3-dihydro-2H- 8.74 (bs, 1H), 7.89-7.91 (m, 2H), 7.74-7.79 (M + H)⁺ isoindole-2- (m, 2H), 7.71-7.75 (m, 2H), 7.37-7.41 (m, carboxamide 2H), 7.33-7.36 (m, 2H), 7.18-7.22 (m, 2H), 4.80-4.81 (bs, 4H) 190 N-(4-{[2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (diethylamino)ethyl] Oxide, Temp = 90° C.) δ ppm 7.78-7.81 (m, m/e 381 carbamoyl}phenyl)- 2H), 7.67-7.70 (m, 2H), 7.37-7.41 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.32-7.36 (m, 2H), 4.82 (s, 4H), 3.66 (t, J = isoindole-2- 6.4 Hz, 2H), 3.29-3.33 (m, 2H), 3.24 (q, J = carboxamide 7.5 Hz, 4H), 1.24-1.33 (m, 6H) 191 N-{4-[2-hydroxy-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) phenylethyl)(methyl) Temp = 90° C.) δ ppm 8.21 (d, J = 1.6 Hz, 1H), m/e 416 carbamoyl]phenyl}- 7.85-7.88 (m, 2H), 7.56-7.59 (m, 2H), 7.51- (M + H)⁺ 1,3-dihydro-2H- 7.54 (m, 2H), 7.29-7.35 (m, 2H), 7.20-7.24 isoindole-2- (m, 3H), 7.14-7.19 (m, 2H), 5.29-5.35 (m, carboxamide 1H), 4.84 (s, 4H), 3.11 (s, 3H) 192 N-{4-[(2- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) aminophenyl)carbamoyl]phenyl}- Oxide) δ ppm 7.91-7.93 (m, 2H), 7.69-7.72 m/e 371 1,3-dihydro-2H- (m, 2H), 7.38-7.43 (m, 2H), 7.33-7.36 (m, (M − H)⁻ isoindole-2- 2H), 7.15-7.18 (m, 1H), 7.01 (ddd, J = 8.0, carboxamide 7.3, 1.5 Hz, 1H), 6.82 (dd, J = 8.0, 1.4 Hz, 1H), 6.66 (td, J = 7.5, 1.5 Hz, 1H), 4.81 (s, 4H) 193 N-(4-{[(2R)-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxypropyl]carbamoyl}phenyl)- Temp = 90° C.) δ ppm 8.28-8.30 (bs, 1H), 8.05- m/e 340 1,3-dihydro-2H- 8.10 (m, 2H), 8.04-8.09 (m, 1H), 7.88-7.91 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.16-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 4.25 (dqd, J = 6.9, 6.2, 4.2 Hz, 1H), 3.78 (ddd, J = 13.4, 6.1, 4.2 Hz, 1H), 3.61 (ddd, J = 13.4, 6.9, 5.4 Hz, 1H), 1.31 (d, J = 6.2 Hz, 3H) 194 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) amino-4-methyl-1- Oxide, Temp = 90° C.) δ ppm 7.80-7.83 (m, m/e 393 oxopentan-2- 2H), 7.65-7.68 (m, 2H), 7.36-7.41 (m, 2H), (M − H)⁻ yl]carbamoyl}phenyl)- 7.31-7.36 (m, 2H), 4.82 (s, 4H), 4.50 (dd, J = 1,3-dihydro-2H- 9.1, 5.0 Hz, 1H), 1.60-1.77 (m, 3H), 0.94 isoindole-2- (dd, J = 11.0, 6.1 Hz, 6H) carboxamide 195 tert-butyl(1-{4- ¹H NMR (400 MHz, pyridine-d₅) δ ppm 1.49- (ESI(+)) [(1,3-dihydro-2H- 1.51 (m, 9H), 1.51-1.61 (m, 1H), 1.88- m/e 465 isoindol-2- 2.00 (m, 1H), 2.98-3.11 (m, 2H), 3.75- (M + H)⁺ ylcarbonyl)amino]ben- 3.90 (m, 1H), 4.21 (d, J = 13.4 Hz, 1H), 4.85 zoyl}piperidin-4- (s, 4H), 6.59 (d, J = 6.1 Hz, 1H), 7.10-7.25 yl)carbamate (m, 5H), 7.45-7.55 (m, 4H), 7.89 (d, J = 8.5 Hz, 2H), 8.26 (s, 1H) 8.64 (s, 1H) 196 N-(4-{[3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (morpholin-4- Oxide, Temp = 90° C.) δ ppm 7.75-7.78 (m, m/e 409 yl)propyl]carbamoyl}phenyl)- 2H), 7.63-7.66 (m, 2H), 7.26-7.42 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 4.79 (s, 4H), 3.82-3.86 (m, 4H), 3.37 (t, J = isoindole-2- 6.6 Hz, 2H), 3.20-3.26 (m, 4H), 3.12-3.18 carboxamide (m, 2H), 1.89-2.03 (m, 2H) 197 N-[4-({4-[3-chloro-5- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57- (ESI(+)) (trifluoromethyl)pyridin- 8.59 (m, 1H), 8.55-8.57 (bs, 1H), 8.23 (d, J = m/e 530 2-yl]piperazin-1- 2.2 Hz, 1H), 7.65-7.69 (m, 2H), 7.37-7.41 (M + H)⁺ yl}carbonyl)phenyl]- (m, 2H), 7.29-7.38 (m, 4H), 4.79-4.80 (bs, 1,3-dihydro-2H- 4H), 3.59-3.84 (m, 4H), 3.45-3.58 (m, 4H) isoindole-2- carboxamide 198 N-(4-{[4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) (cyclohexylmethyl)piperazin- Temp = 90° C.) δ ppm 8.31-8.33 (bs, 1H), 7.91- m/e 445 1yl]carbony1}phenyl)- 7.95 (m, 2H), 7.50-7.57 (m, 2H), 7.20-7.23 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.86 (s, 4H), isoindole-2- 3.63-3.74 (m, 4H), 2.40-2.43 (m, 4H), 2.16 carboxamide (d, J = 7.0 Hz, 2H), 1.75-1.81 (m, 2H), 1.56- 1.70 (m, 3H), 1.43-1.56 (m, 1H), 1.09-1.29 (m, 3H), 0.82-0.97 (m, 2H) 199 N-(4-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.28 (ESI(−)) chlorobenzyl)-1H- (s, 1H), 8.64 (s, 1H), 8.18 (s, 1H), 7.85-7.89 m/e 470 pyrazol-4- (m, 2H), 7.70-7.74 (m, 2H), 7.63 (s, 1H), (M − H)⁻ yl]carbamoyl}phenyl)- 7.28-7.42 (m, 7H), 7.18-7.23 (m, 1H), 5.33- 1,3-dihydro-2H- 5.34 (bs, 2H), 4.79-4.81 (bs, 4H) isoindole-2- carboxamide 200 N-(4-{[3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) (diethylcarbamoyl)piperidin-1- Temp = 90° C.) δ ppm 8.27-8.29 (bs, 1H), 7.89- m/e 447 yl]carbonyl}phenyl)- 7.92 (m, 2H), 7.52-7.56 (m, 2H), 7.19-7.24 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 4.17-4.21 (m, 1H), 3.19-3.43 (m, 5H), 2.94 carboxamide (ddd, J = 13.0, 12.1, 3.3 Hz, 0H), 2.84 (tt, J = 10.6, 4.1 Hz, 1H), 1.89-2.07 (m, 2H), 1.58- 1.66 (m, 1H), 1.43-1.58 (m, 1H), 1.04 (t, J = 7.1 Hz, 6H) 201 N-(4-{[3-(piperidin-1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) yl)propyl]carbamoyl}phenyl)- Temp = 90° C.) δ ppm 8.45-8.51 (m, 1H), 8.32- m/e 407 1,3-dihydro-2H- 8.36 (bs, 1H), 8.16-8.18 (m, 2H), 7.93-7.96 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.24 (m, 2H), 7.15-7.19 (m, carboxamide 2H), 4.85 (s, 4H), 3.61 (q, J = 6.1 Hz, 2H), 3.00-3.05 (m, 2H), 2.88-2.91 (m, 4H), 2.08- 2.16 (m, 2H), 1.66-1.76 (m, 4H), 1.32-1.41 (m, 2H) 202 N-(4-{[4-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.53 (ESI(+)) hydroxyethyl)piperazin-1- (s, 1H), 7.62-7.66 (m, 2H), 7.24-7.43 (m, m/e 395 yl]carbonyl}phenyl)- 6H), 4.78-4.79 (bs, 4H), 4.39-4.44 (m, 1H), (M + H)⁺ 1,3-dihydro-2H- 3.39-3.58 (m, 6H), 2.34-2.45 (m, 6H) isoindole-2- carboxamide 203 N-{4-[(2-hydroxy-6- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylphenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 9.59-9.61 (bs, 1H), 8.38- m/e 388 1,3-dihydro-2H- 8.40 (bs, 1H), 8.22-8.25 (m, 2H), 7.95-7.98 (M + H)⁺ isoindole-2- (m, 2H), 7.20-7.23 (m, 2H), 7.16-7.19 (m, carboxamide 2H), 7.08 (d, J = 7.1 Hz, 1H), 7.06 (d, J = 2.0 Hz, 1H), 6.82 (dd, J = 7.0, 1.8 Hz, 1H), 4.85 (s, 4H), 2.43 (s, 3H) 204 N-(4-{[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (dimethylamino)bu- Oxide, Temp = 90° C.) δ ppm 7.76-7.79 (m, m/e 381 tyl]carbamoyl}phenyl)- 2H), 7.64-7.67 (m, 2H), 7.37-7.42 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.32-7.36 (m, 2H), 4.82 (s, 4H), 3.32-3.37 isoindole-2- (m, 2H), 3.10-3.15 (m, 2H), 2.81 (s, 6H), carboxamide 1.68-1.79 (m, 2H), 1.59-1.67 (m, 2H) 205 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) hydroxypropyl)carbamoyl]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.75-7.77 (m, m/e 340 1,3-dihydro-2H- 2H), 7.63-7.65 (m, 2H), 7.36-7.41 (m, 2H), (M + H)⁺ isoindole-2- 7.31-7.36 (m, 2H), 4.82 (s, 4H), 3.53 (t, J = carboxamide 6.3 Hz, 2H), 3.36 (t, J = 6.9 Hz, 2H), 1.74 (p, J = 6.6 Hz, 2H) 206 N-{4-[(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) cyclohexylpiperazin- Temp = 90° C.) δ ppm 8.31-8.33 (bs, 1H), 7.91- m/e 433 1- 7.94 (m, 2H), 7.52-7.56 (m, 2H), 7.20-7.25 (M + H)⁺ yl)carbonyl]phenyl}- (m, 2H), 7.15-7.20 (m, 2H), 4.86 (s, 4H), 1,3-dihydro-2H- 3.72-3.80 (m, 4H), 2.62-2.65 (m, 4H), 2.36- isoindole-2- 2.44 (m, 1H), 1.80-1.84 (m, 2H), 1.67-1.72 carboxamide (m, 2H), 1.48-1.54 (m, 1H), 1.01-1.28 (m, 5H) 207 N-[4-(5,6- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (ESI(+)) dihydro[1,2,4]triazolo[4,3- (s, 1H), 8.51 (s, 1H), 7.72 (s, 1H), 7.68-7.70 m/e 389 a]pyrazin-7(8H)- (m, 1H), 7.41-7.47 (m, 2H), 7.35-7.40 (m, (M + H)⁺ ylcarbonyl)phenyl]- 2H), 7.29-7.35 (m, 2H), 4.86 (s, 2H), 4.79- 1,3-dihydro-2H- 4.80 (bs, 4H), 4.15 (t, J = 5.3 Hz, 2H), 3.83- isoindole-2- 3.95 (m, 2H) carboxamide 208 N-{4-[methyl(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.49- (ESI(+)) methylbutyl)carbamoyl]phenyl}- 8.53 (bs, 1H), 7.60-7.67 (m, 2H), 7.26-7.40 m/e 366 1,3-dihydro-2H- (m, 6H), 4.78 (s, 4H), 3.16-3.49 (m, 2H), (M + H)⁺ isoindole-2- 2.92 (s, 3H), 1.13-1.79 (m, 3H), 0.48-1.12 carboxamide (m, 6H) 209 N-[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (propylcarbamoyl)phenyl]- Oxide, Temp = 90° C.) δ ppm 7.75-7.78 (m, m/e 324 1,3-dihydro- 2H), 7.62-7.65 (m, 2H), 7.32-7.40 (m, 4H), (M + H)⁺ 2H-isoindole-2- 4.82 (s, 4H), 3.22-3.30 (m, 2H), 1.53-1.63 carboxamide (m, 2H), 0.93 (t, J = 7.4 Hz, 3H) 210 N-(4-{[(2S)-1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxybutan-2- Temp = 90° C.) δ ppm 8.28-8.29 (bs, 1H), 8.06- m/e 354 yl]carbamoyl}phenyl)- 8.08 (m, 2H), 7.87-7.90 (m, 2H), 7.57-7.61 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 7.19-7.23 (m, 2H), 7.15-7.19 (m, isoindole-2- 2H), 4.84 (s, 4H), 4.37-4.47 (m, 1H), 3.91- carboxamide 3.99 (m, 2H), 1.84-1.96 (m, 1H), 1.71-1.85 (m, 1H), 1.03 (t, J = 7.5 Hz, 3H) 211 N-{4-[(5- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) fluoropyridin-2- Temp = 90° C.) δ ppm 10.45-10.47 (bs, 1H), m/e 377 yl)carbamoyl]phenyl}- 8.58 (dd, J = 9.1, 4.2 Hz, 1H), 8.42-8.44 (bs, (M + H)⁺ 1,3-dihydro-2H- 1H), 8.24 (d, J = 3.0 Hz, 1H), 8.18-8.20 (m, isoindole-2- 2H), 7.98-8.00 (m, 2H), 7.45 (ddd, J = 9.0, carboxamide 8.1, 3.1 Hz, 1H), 7.20-7.24 (m, 2H), 7.15- 7.20 (m, 2H), 4.86 (s, 4H) 212 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) [(cyclopropylmethyl) Temp = 90° C.) δ ppm 8.23-8.24 (bs, 1H), 7.90- m/e 378 (propyl)carbamoyl]phenyl}- 7.92 (m, 2H), 7.48-7.52 (m, 2H), 7.19-7.24 (M + H)⁺ 1,3-dihydro- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), 2H-isoindole-2- 3.49-3.53 (m, 2H), 3.35 (d, J = 6.7 Hz, 2H), carboxamide 1.58-1.66 (m, 2H), 0.96-1.07 (m, 1H), 0.81 (t, J = 7.4 Hz, 3H), 0.42-0.47 (m, 2H), 0.15- 0.19 (m, 2H) 213 N-(4-{[(2S)-1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxypropan-2- Temp = 90° C.) δ ppm 8.28-8.34 (m, 1H), 8.05- m/e 354 yl]carbamoyl}phenyl)- 8.08 (m, 2H), 7.88-7.90 (m, 2H), 7.54-7.63 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 7.18-7.24 (m, 2H), 7.15-7.18 (m, isoindole-2- 2H), 4.83 (s, 4H), 4.54-4.64 (m, 1H), 3.53 carboxamide (dd, J = 9.5, 5.2 Hz, 1H), 3.45 (dd, J = 9.5, 5.5 Hz, 1H), 3.27 (s, 3H), 1.30 (d, J = 6.8 Hz, 3H) 214 N-[4-(1,3,4,9- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) tetrahydro-2H-beta- Temp = 90° C.) δ ppm 11.10-11.13 (bs, 1H), m/e 437 carbolin-2- 8.29-8.30 (bs, 1H), 7.91-7.94 (m, 2H), 7.57- (M + H)⁺ ylcarbonyl)phenyl]- 7.61 (m, 2H), 7.57-7.60 (m, 1H), 7.45-7.48 1,3-dihydro-2H- (m, 1H), 7.16-7.25 (m, 6H), 4.96-4.97 (bs, isoindole-2- 2H), 4.87 (s, 4H), 3.86-3.92 (m, 2H), 2.85 (t, carboxamide J = 5.7 Hz, 2H) 215 N-[4-(tert- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) butylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.24-8.26 (bs, 1H), 7.96- m/e 338 1,3-dihydro-2H- 7.99 (m, 2H), 7.85-7.88 (m, 2H), 7.19-7.23 (M + H)⁺ isoindole-2- (m, 2H), 7.14-7.19 (m, 2H), 6.93-6.96 (bs, carboxamide 1H), 4.83 (s, 4H), 1.52 (s, 9H) 216 N-[4-({4-[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (trifluoromethyl)phe- Oxide) δ ppm 7.64-7.67 (m, 2H), 7.53-7.55 m/e 495 nyl]piperazin-1- (m, 2H), 7.36-7.42 (m, 4H), 7.31-7.36 (m, (M + H)⁺ yl}carbonyl)phenyl]- 2H), 7.09-7.11 (m, 2H), 4.79-4.80 (bs, 4H), 1,3-dihydro-2H- 3.55-3.76 (m, 4H), 3.26-3.43 (m, 4H) isoindole-2- carboxamide 217 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylbutan-2- Temp = 90° C.) δ ppm 8.28-8.29 (bs, 1H), 8.06- m/e 352 yl)carbamoyl]phenyl}- 8.09 (m, 2H), 7.88-7.92 (m, 2H), 7.30-7.35 (M + H)⁺ 1,3-dihydro-2H- (bs, 1H), 7.19-7.24 (m, 2H), 7.14-7.18 (m, isoindole-2- 2H), 4.84 (s, 4H), 4.22-4.32 (m, 1H), 1.82- carboxamide 1.91 (m, 1H), 1.19 (d, J = 6.8 Hz, 3H), 0.97 (d, J = 6.7 Hz, 3H), 0.93 (d, J = 6.7 Hz, 3H) 218 N-{4-[(3,3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) difluoropyrrolidin-1- Temp = 90° C.) δ ppm 8.34-8.36 (bs, 1H), 7.91- m/e 370 yl)carbonyl]phenyl}- 7.94 (m, 2H), 7.61-7.65 (m, 2H), 7.20-7.24 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.86 (s, 4H), isoindole-2- 3.96-4.04 (m, 2H), 3.76 (t, J = 7.4 Hz, 2H), carboxamide 2.21-2.35 (m, 2H) 219 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylpiperidin-1- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 7.90- m/e 364 yl)carbonyl]phenyl}- 7.92 (m, 2H), 7.47-7.51 (m, 2H), 7.19-7.23 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.14-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 4.62-4.67 (m, 1H), 4.02-4.17 (m, 1H), 2.93 carboxamide (td, J = 12.9, 3.1 Hz, 1H), 1.30-1.65 (m, 6H), 1.14 (d, J = 6.9 Hz, 3H) 220 N-(4-{[(3S)-1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) benzylpyrrolidin-3- Temp = 90° C.) δ ppm 8.26-8.31 (bs, 1H), 8.20- m/e 439 yl]carbamoyl}phenyl)- 8.26 (m, 1H), 8.09-8.12 (m, 2H), 7.89-7.92 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.41-7.48 (m, 2H), 7.23-7.33 (m, isoindole-2- 3H), 7.19-7.24 (m, 2H), 7.14-7.19 (m, 2H), carboxamide 4.90-5.00 (m, 1H), 4.84 (s, 4H), 3.91 (s, 2H), 3.09-3.17 (m, 3H), 2.68-2.75 (m, 1H), 2.30- 2.43 (m, 1H), 2.02 (dtd, J = 13.1, 7.8, 5.2 Hz, 1H) 221 N-{4-[(4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxypiperidin-1- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 7.89- m/e 366 yl)carbonyl]phenyl}- 7.92 (m, 2H), 7.52-7.56 (m, 2H), 7.19-7.23 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.16-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 3.99-4.12 (m, 3H), 3.35 (ddd, J = 13.2, 9.1, carboxamide 3.8 Hz, 2H), 1.82-1.98 (m, 2H), 1.59-1.75 (m, 2H) 222 N-{4-[bis(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.22-8.24 (bs, 1H), 7.88- m/e 398 1,3-dihydro-2H- 7.92 (m, 2H), 7.54-7.57 (m, 2H), 7.19-7.23 (M + H)⁺ isoindole-2- (m, 2H), 7.16-7.18 (m, 2H), 4.84 (s, 4H), carboxamide 3.75 (t, J = 5.8 Hz, 4H), 3.57 (t, J = 5.8 Hz, 4H), 3.23 (s, 6H) 223 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) fluorophenyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 10.17-10.23 (m, 1H), m/e 376 1,3-dihydro-2H- 8.35-8.36 (bs, 1H), 8.12-8.14 (m, 2H), 8.04 (M + H)⁺ isoindole-2- (dt, J = 11.5, 2.3 Hz, 1H), 7.90-7.93 (m, 2H), carboxamide 7.66 (ddd, J = 8.1, 2.0, 1.0 Hz, 1H), 7.20- 7.31 (m, 3H), 7.15-7.19 (m, 2H), 6.83 (tdd, J = 8.4, 2.6, 0.9 Hz, 1H), 4.84 (s, 4H) 224 N-[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (cyclopentylcarbamoyl)phenyl]- Oxide) δ ppm 7.76-7.78 (m, 2H), 7.60-7.68 m/e 350 1,3-dihydro-2H- (m, 2H), 7.37-7.42 (m, 2H), 7.32-7.35 (m, (M + H)⁺ isoindole-2- 2H), 4.76-4.82 (m, 4H), 4.17-4.25 (m, 1H), carboxamide 1.86-1.93 (m, 2H), 1.66-1.71 (m, 2H), 1.50- 1.59 (m, 4H) 225 N-{4-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) carbamoylpiperidin-1- Oxide, Temp = 90° C.) δ ppm 7.62-7.64 (m, m/e 393 yl)carbonyl]phenyl}- 2H), 7.30-7.40 (m, 6H), 4.81 (s, 4H), 4.01- (M − H)⁻ 1,3-dihydro-2H- 4.09 (m, 2H), 2.96-3.04 (m, 2H), 2.42-2.50 isoindole-2- (m, 1H), 1.76-1.82 (m, 2H), 1.51-1.62 (m, carboxamide 2H) 226 N-[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) (cyclopropylcarbamoyl)phenyl]- Oxide) δ ppm 7.73-7.76 (m, 2H), 7.60-7.67 m/e 320 1,3-dihydro-2H- (m, 2H), 7.36-7.40 (m, 2H), 7.32-7.36 (m, (M − H)⁻ isoindole-2- 2H), 4.78-4.79 (bs, 4H), 2.79-2.84 (m, 1H), carboxamide 0.67-0.75 (m, 2H), 0.53-0.60 (m, 2H) 227 N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) (methylcarbamoyl)phenyl]- (s, 1H), 8.19-8.26 (m, 1H), 7.73-7.77 (m, m/e 296 1,3-dihydro- 2H), 7.63-7.67 (m, 2H), 7.30-7.39 (m, 4H), (M + H)⁺ 2H-isoindole-2- 4.79 (s, 4H), 2.76 (d, J = 4.5 Hz, 3H) carboxamide 228 N-(4-{[3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (dimethylamino)pro- Oxide, Temp = 90° C.) δ ppm 7.77-7.80 (m, m/e 367 pyl]carbamoyl}phenyl)- 2H), 7.65-7.68 (m, 2H), 7.37-7.44 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.32-7.36 (m, 2H), 4.82 (s, 4H), 3.39 (t, J = isoindole-2- 6.7 Hz, 2H), 3.09-3.19 (m, 2H), 2.83 (s, 6H), carboxamide 1.89-2.03 (m, 2H) 229 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) [methyl(tetrahydrofuran-2- Temp = 90° C.) δ ppm 8.24-8.26 (bs, 1H), 7.89- m/e 380 ylmethyl)carbamoyl] 7.91 (m, 2H), 7.52-7.56 (m, 2H), 7.19-7.24 (M + H)⁺ phenyl}-1,3-dihydro- (m, 2H), 7.14-7.19 (m, 2H), 4.85 (s, 4H), 2H-isoindole-2- 4.09-4.20 (m, 1H), 3.72-3.78 (m, 1H), 3.59- carboxamide 3.71 (m, 2H), 3.46-3.52 (m, 1H), 3.10 (s, 3H), 1.74-1.86 (m, 1H), 1.62-1.72 (m, 2H), 1.39-1.50 (m, 1H) 230 N-[4-(pentan-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) ylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 8.07- m/e 352 1,3-dihydro-2H- 8.10 (m, 2H), 7.88-7.91 (m, 2H), 7.44 (d, J = (M + H)⁺ isoindole-2- 7.0 Hz, 1H), 7.19-7.23 (m, 2H), 7.14-7.18 carboxamide (m, 2H), 4.84 (s, 4H), 4.35-4.45 (m, 1H), 1.58-1.67 (m, 1H), 1.34-1.56 (m, 3H), 1.24 (d, J = 6.6 Hz, 3H), 0.88 (t, J = 7.2 Hz, 3H) 231 N-[4-(pentan-3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) ylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.27-8.29 (bs, 1H), 8.08- m/e 352 1,3-dihydro-2H- 8.11 (m, 2H), 7.89-7.91 (m, 2H), 7.31-7.37 (M + H)⁺ isoindole-2- (m, 1H), 7.19-7.23 (m, 2H), 7.14-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 4.15-4.24 (m, 1H), 1.42- 1.72 (m, 4H), 0.96 (t, J = 7.4 Hz, 6H) 232 N-[4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) (cyclobutylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.25-8.27 (m, 1H), 8.06- m/e 336 1,3-dihydro-2H- 8.10 (m, 2H), 7.92-8.00 (m, 1H), 7.88-7.90 (M + H)⁺ isoindole-2- (m, 2H), 7.19-7.23 (m, 2H), 7.14-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 4.71-4.80 (m, 1H), 2.27- 2.46 (m, 2H), 1.99-2.17 (m, 2H), 1.53-1.74 (m, 2H) 233 N-{4-[(1,3-dioxolan-2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) ylmethyl)(methyl)carbamoyl]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.61-7.64 (m, m/e 280 1,3-dihydro-2H- 2H), 7.31-7.45 (m, 6H), 5.04 (t, J = 4.3 Hz, (M − H)⁻ isoindole-2- 1H), 4.81 (s, 4H), 3.88-3.94 (m, 2H), 3.82- carboxamide 3.86 (m, 2H), 3.54 (d, J = 4.3 Hz, 2H), 3.04 (s, 3H) 234 N-(4-{[1-(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.45 (ESI(+)) fluorophenyl)-1H- (s, 1H), 8.65-8.68 (m, 2H), 7.82-7.94 (m, m/e 442 pyrazol-4- 5H), 7.74-7.78 (m, 2H), 7.31-7.40 (m, 6H), (M + H)⁺ yl]carbamoyl}phenyl)- 4.80-4.82 (bs, 4H) 1,3-dihydro-2H- isoindole-2- carboxamide 235 N-{4-[(1-hydroxy-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) methylpropan-2- Temp = 90° C.) δ ppm 8.23-8.34 (m, 1H), 7.95- m/e 352 yl)carbamoyl]phenyl}- 7.97 (m, 2H), 7.84-7.88 (m, 2H), 7.19-7.24 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.15-7.18 (m, 2H), 4.83 (s, 4H), isoindole-2- 3.91 (s, 2H), 1.59 (s, 6H) carboxamide 236 N-{4-[(1-phenyl-1H- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.45 (ESI(+)) pyrazol-4- (s, 1H), 8.67 (s, 2H), 7.90-7.95 (m, 3H), m/e 424 yl)carbamoyl]phenyl}- 7.80-7.84 (m, 2H), 7.74-7.78 (m, 2H), 7.47- (M + H)⁺ 1,3-dihydro-2H- 7.53 (m, 2H), 7.27-7.40 (m, 5H), 4.80-4.82 isoindole-2- (bs, 4H) carboxamide 237 N-[4-({2-[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) (trifluoromethyl)phe- Oxide) δ ppm 7.72-7.74 (m, 2H), 7.63-7.67 m/e 452 nyl]ethyl}carbamoyl) (m, 4H), 7.48-7.50 (m, 2H), 7.36-7.41 (m, (M − H)⁻ phenyl]-1,3-dihydro- 2H), 7.31-7.36 (m, 2H), 4.78-4.79 (bs, 4H), 2H-isoindole-2- 3.52 (t, J = 7.0 Hz, 2H), 2.95 (t, J = 7.2 Hz, carboxamide 2H) 238 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) methoxyethyl)(pro- Temp = 90° C.) δ ppm 8.24-8.26 (bs, 1H), 7.89- m/e 380 pyl)carbamoyl]phenyl}- 7.92 (m, 2H), 7.49-7.53 (m, 2H), 7.19-7.23 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 3.65 (t, J = 5.7 Hz, 2H), 3.56 (t, J = 5.7 Hz, carboxamide 2H), 3.46 (t, J = 7.3 Hz, 2H), 3.24 (s, 3H), 1.53-1.67 (m, 2H), 0.78 (t, J = 7.4 Hz, 3H) 239 N-[4-(sec- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) butylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 8.06- m/e 338 1,3-dihydro-2H- 8.10 (m, 2H), 7.88-7.91 (m, 2H), 7.42-7.46 (M + H)⁺ isoindole-2- (m, 1H), 7.19-7.23 (m, 2H), 7.15-7.18 (m, carboxamide 2H), 4.84 (s, 4H), 4.21-4.36 (m, 1H), 1.42- 1.75 (m, 2H), 1.23 (d, J = 6.6 Hz, 3H), 0.93 (t, J = 7.4 Hz, 3H) 240 N-(4-{[3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(−)) (trifluoromethyl)piperidin-1- Oxide) δ ppm 8.61-8.63 (bs, 1H), 7.63-7.65 m/e 416 yl]carbonyl}phenyl)- (m, 2H), 7.36-7.41 (m, 2H), 7.31-7.36 (m, (M − H)⁻ 1,3-dihydro-2H- 4H), 4.78-4.79 (bs, 4H), 3.94-4.64 (m, 2H), isoindole-2- 2.97-3.12 (m, 2H), 1.97-2.02 (m, 1H), 1.64- carboxamide 1.83 (m, 1H), 1.55-1.66 (m, 1H), 1.42-1.55 (m, 1H) 241 N-{4-[bis(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) ethoxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.20-8.22 (bs, 1H), 7.89- m/e 424 1,3-dihydro-2H- 7.92 (m, 2H), 7.57-7.60 (m, 2H), 7.19-7.23 (M − H)⁻ isoindole-2- (m, 2H), 7.14-7.19 (m, 2H), 4.84 (s, 4H), carboxamide 3.77 (t, J = 5.8 Hz, 4H), 3.62-3.65 (m, 4H), 3.42 (q, J = 7.0 Hz, 4H), 1.11 (t, J = 7.0 Hz, 6H) 242 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) [butyl(ethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.23-8.25 (bs, 1H), 7.89- m/e 366 1,3-dihydro-2H- 7.93 (m, 2H), 7.48-7.51 (m, 2H), 7.19-7.23 (M + H)⁺ isoindole-2- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), carboxamide 3.35-3.47 (m, 4H), 1.56 (p, J = 7.3 Hz, 2H), 1.19-1.32 (m, 2H), 1.10 (t, J = 7.1 Hz, 3H), 0.83 (t, J = 7.3 Hz, 3H) 243 N-{4-[(1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxypropan-2- Temp = 90° C.) δ ppm 8.28-8.32 (m, 1H), 8.05- m/e 354 yl)carbamoyl]phenyl}- 8.08 (m, 2H), 7.88-7.90 (m, 2H), 7.56-7.60 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 7.19-7.24 (m, 2H), 7.15-7.19 (m, isoindole-2- 2H), 4.84 (s, 4H), 4.54-4.64 (m, 1H), 3.53 carboxamide (dd, J = 9.6, 5.2 Hz, 1H), 3.45 (dd, J = 9.5, 5.5 Hz, 1H), 3.27 (s, 3H), 1.30 (d, J = 6.7 Hz, 3H) 244 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyethyl)(meth- Temp = 90° C.) δ ppm 8.23-8.28 (bs, 1H), 7.88- m/e 354 yl)carbamoyl]phenyl}- 7.91 (m, 2H), 7.51-7.56 (m, 2H), 7.19-7.25 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 3.63 (t, J = 5.6 Hz, 2H), 3.53 (t, J = 5.6 Hz, carboxamide 2H), 3.23 (s, 3H), 3.04 (s, 3H) 245 N-{4-[(3R)- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) tetrahydrofuran-3- Temp = 90° C.) δ ppm 8.29-8.31 (bs, 1H), 8.04- m/e 350 ylcarbamoyl]phenyl}- 8.09 (m, 2H), 7.97-8.04 (m, 1H), 7.88-7.90 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.19-7.24 (m, 2H), 7.14-7.19 (m, isoindole-2- 2H), 4.80-4.87 (m, 1H), 4.80-4.87 (m, 4H), carboxamide 4.02 (dd, J = 9.0, 6.1 Hz, 1H), 3.85-3.93 (m, 2H), 3.72 (td, J = 8.2, 6.1 Hz, 1H), 2.21 (tdd, J = 7.9, 12.7, 6.4 Hz, 1H), 1.93-2.02 (m, 1H) 246 N-[4-(morpholin-4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) ylcarbonyl)phenyl]- Oxide, Temp = 90° C.) δ ppm 7.62-7.65 (m, m/e 350 1,3-dihydro-2H- 2H), 7.31-7.41 (m, 6H), 4.81 (s, 4H), 3.63- (M − H)⁻ isoindole-2- 3.65 (m, 4H), 3.50-3.58 (m, 4H) carboxamide 247 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) [isobutyl(methyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.24-8.26 (bs, 1H), 7.89- m/e 352 1,3-dihydro-2H- 7.92 (m, 2H), 7.48-7.52 (m, 2H), 7.19-7.24 (M + H)⁺ isoindole-2- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), carboxamide 3.30 (d, J = 7.3 Hz, 2H), 2.94 (s, 3H), 1.91- 2.07 (m, 1H), 0.83 (d, J = 6.6 Hz, 6H) 248 N-[4-({4-[2-(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) hydroxyethoxy)ethyl]piperazin-1- Oxide, Temp = 90° C.) δ ppm 7.66-7.69 (m, m/e 439 yl}carbonyl)phenyl]- 2H), 7.39-7.43 (m, 2H), 7.36-7.40 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.32-7.36 (m, 2H), 4.82 (s, 4H), 3.79-3.83 isoindole-2- (m, 2H), 3.71-3.90 (m, 4H), 3.58-3.63 (m, carboxamide 2H), 3.53-3.58 (m, 2H), 3.32-3.35 (m, 2H), 3.22 (s, 4H) 249 N-{4-[(3- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylpiperidin-1- Temp = 90° C.) δ ppm 8.25-8.27 (bs, 1H), 7.90- m/e 364 yl)carbonyl]phenyl}- 7.92 (m, 2H), 7.51-7.55 (m, 2H), 7.19-7.23 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 4.09-4.19 (m, 2H), 2.88 (ddd, J = 13.1, 11.1, carboxamide 3.2 Hz, 1H), 2.57 (dd, J = 12.9, 10.1 Hz, 1H), 1.63-1.69 (m, 1H), 1.47-1.61 (m, 2H), 1.34-1.45 (m, 1H), 1.03 (dddd, J = 13.0, 11.3, 10.6, 4.4 Hz, 1H), 0.75 (d, J = 6.6 Hz, 3H) 250 N-(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) carbamoylphenyl)- (s, 1H), 7.76-7.83 (m, 2H), 7.73-7.85 (bs, m/e 282 1,3-dihydro-2H- 1H), 7.63-7.67 (m, 2H), 7.30-7.39 (m, 4H), (M + H)⁺ isoindole-2- 7.09-7.19 (bs, 1H), 4.79 (s, 4H) carboxamide 251 N-(4-{[(2S)-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) (trifluoromethyl)pyrrolidin-1- Temp = 90° C.) δ ppm 8.34-8.36 (bs, 1H), 7.91- m/e 402 yl]carbonyl}phenyl)- 7.93 (m, 2H), 7.65-7.68 (m, 2H), 7.20-7.25 (M − H)⁻ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 5.25-5.34 (m, isoindole-2- 1H), 4.85 (s, 4H), 3.50-3.56 (m, 2H), 1.95- carboxamide 2.02 (m, 2H), 1.80-1.89 (m, 1H), 1.58-1.70 (m, 1H) 252 N-(4-{[(2S)-1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxy-4- Temp = 90° C.) δ ppm 8.29-8.30 (bs, 1H), 8.06- m/e 382 methylpentan-2- 8.11 (m, 2H), 7.88-7.90 (m, 2H), 7.62 (d, J = (M + H)⁺ yl]carbamoyl}phenyl)- 8.0 Hz, 1H), 7.19-7.24 (m, 2H), 7.14-7.18 1,3-dihydro-2H- (m, 2H), 4.84 (s, 4H), 4.58-4.67 (m, 1H), isoindole-2- 3.95 (d, J = 4.9 Hz, 3H), 1.82-1.93 (m, 1H), carboxamide 1.73 (ddd, J = 14.0, 8.6, 5.5 Hz, 1H), 1.68 (ddd, J = 13.7, 8.2, 5.5 Hz, 1H), 0.99 (d, J = 6.6 Hz, 3H), 0.93 (d, J = 6.6 Hz, 3H) 253 N-(4-{[(1R)-2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxy-1- Temp = 90° C.) δ ppm 8.29-8.30 (bs, 1H), 8.15- m/e 402 phenylethyl]carbamoyl}phenyl)- 8.18 (m, 1H), 8.08-8.11 (m, 2H), 7.87-7.90 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.61-7.64 (m, 2H), 7.27-7.33 (m, isoindole-2- 2H), 7.19-7.24 (m, 3H), 7.15-7.19 (m, 2H), carboxamide 5.68-5.73 (m, 1H), 4.83 (s, 4H), 4.23 (d, J = 5.6 Hz, 2H) 254 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methylpyrrolidin-1- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 7.89- m/e 350 yl)carbonyl]phenyl}- 7.92 (m, 2H), 7.60-7.65 (m, 2H), 7.20-7.24 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.86 (s, 4H), isoindole-2- 4.26-4.36 (m, 1H), 3.47 (t, J = 6.8 Hz, 2H), carboxamide 1.92 (dq, J = 12.2, 7.1 Hz, 1H), 1.67-1.78 (m, 1H), 1.52-1.63 (m, 1H), 1.41 (dtd, J = 12.2, 6.9, 5.2 Hz, 1H), 1.22 (d, J = 6.2 Hz, 3H) 255 N-{4-[ethyl(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) methoxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.24-8.26 (bs, 1H), 7.89- m/e 368 1,3-dihydro-2H- 7.91 (m, 2H), 7.49-7.53 (m, 2H), 7.19-7.24 (M + H)⁺ isoindole-2- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), carboxamide 3.62-3.66 (m, 2H), 3.53-3.58 (m, 2H), 3.50 (q, J = 7.1 Hz, 2H), 3.24 (s, 3H), 1.11 (t, J = 7.1 Hz, 3H) 256 N-(4-{[(2R)-1- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90 (ESI(+)) hydroxy-3- C.) δ ppm 8.29-8.30 (bs, 1H), 8.05-8.08 (m, m/e 368 methylbutan-2- 2H), 7.87-7.90 (m, 2H), 7.46-7.53 (m, 1H), (M + H)⁺ yl]carbamoyl}phenyl)- 7.19-7.24 (m, 2H), 7.15-7.19 (m, 2H), 4.84 1,3-dihydro-2H- (s, 4H), 4.29-4.36 (m, 1H), 3.99 (d, J = 4.8 isoindole-2- Hz, 2H), 2.19-2.28 (m, 1H), 1.08 (d, J = 2.3 carboxamide Hz, 3H), 1.06 (d, J = 2.4 Hz, 3H) 257 N-{4-[(2,6- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethylmorpholin-4- Temp = 90° C.) δ ppm 8.33-8.40 (m, 1H), 7.92- m/e 380 yl)carbonyl]phenyl}- 7.96 (m, 2H), 7.54-7.58 (m, 2H), 7.19-7.25 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.86 (s, 4H), isoindole-2- 4.14-4.22 (m, 1H), 3.93-4.01 (m, 1H), 3.70 carboxamide (dd, J = 13.0, 3.4 Hz, 1H), 3.51-3.61 (m, 1H), 3.32 (dd, J = 13.0, 6.3 Hz, 1H), 2.64 (dd, J = 13.1, 10.5 Hz, 1H), 1.02-1.15 (m, 6H) 258 N-(4-{[(2R)-1- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) hydroxybutan-2- Temp = 90° C.) δ ppm 8.25-8.31 (m, 1H), 8.05- m/e 354 yl]carbamoyl}phenyl)- 8.08 (m, 2H), 7.87-7.90 (m, 2H), 7.58 (d, J = (M + H)⁺ 1,3-dihydro-2H- 7.5 Hz, 1H), 7.19-7.24 (m, 2H), 7.14-7.19 isoindole-2- (m, 2H), 4.84 (s, 4H), 4.36-4.47 (m, 1H), carboxamide 3.95 (d, J = 4.9 Hz, 2H), 1.85-1.96 (m, 1H), 1.72-1.84 (m, 1H), 1.02 (t, J = 7.4 Hz, 3H) 259 N-{4-[(2,5- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) dimethylpyrrolidin-1- Temp = 90° C.) δ ppm 8.23-8.25 (bs, 1H), 7.90- m/e 364 yl)carbonyl]phenyl}- 7.92 (m, 2H), 7.53-7.62 (m, 2H), 7.19-7.23 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 4.11-4.39 (m, 2H), 1.78-2.11 (m, 2H), 1.35- carboxamide 1.59 (m, 2H), 0.95-1.27 (m, 6H) 260 N-[4-(prop-2-yn-1- ¹H NMR (400 MHz, DMSO-d₆, (ESI(+)) ylcarbamoyl)phenyl]- Temp = 90° C.) δ ppm 3.10 (t, J = 2.38 Hz, 1 H), m/e 320 1,3-dihydro-2H- 4.03 (dd, J = 5.55, 2.78 Hz, 2 H), 4.79 (s, 4 (M + H)⁺ isoindole-2- H), 7.28-7.42 (m, 4 H), 7.64-7.82 (m, 4 carboxamide H), 8.60 (s, 1 H), 8.73 (t, J = 5.55 Hz, 1 H) 261 N-{4-[isopropyl(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(−)) methoxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.26-8.28 (bs, 1H), 7.90- m/e 380 1,3-dihydro-2H- 7.93 (m, 2H), 7.48-7.50 (m, 2H), 7.19-7.23 (M − H)⁻ isoindole-2- (m, 2H), 7.15-7.18 (m, 2H), 4.85 (s, 4H), carboxamide 4.18-4.32 (m, 1H), 3.56-3.68 (m, 4H), 3.26 (s, 3H), 1.13 (d, J = 6.7 Hz, 6H) 262 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) [isopropyl(propyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.24-8.26 (bs, 1H), 7.90- m/e 366 1,3-dihydro-2H- 7.92 (m, 2H), 7.46-7.48 (m, 2H), 7.19-7.23 (M + H)⁺ isoindole-2- (m, 2H), 7.16-7.18 (m, 2H), 4.85 (s, 4H), carboxamide 4.20-4.32 (m, 1H), 3.25-3.30 (m, 2H), 1.59- 1.77 (m, 2H), 1.12-1.17 (m, 6H), 0.82 (t, J = 7.4 Hz, 3H) 263 N-{4-[(2- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) cyanoethyl)(cyclopro- Temp = 90° C.) δ ppm 8.27-8.29 (bs, 1H), 7.90- m/e 375 pyl)carbamoyl]phenyl}- 7.93 (m, 2H), 7.65-7.68 (m, 2H), 7.20-7.23 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.15-7.19 (m, 2H), 4.85 (s, 4H), isoindole-2- 3.81 (t, J = 6.6 Hz, 2H), 2.90-2.96 (m, 1H), carboxamide 2.83 (t, J = 6.6 Hz, 2H), 0.54-0.61 (m, 2H), 0.45-0.52 (m, 2H) 264 N-{4- ¹H NMR (400 MHz, Pyridine-d₅, (ESI(+)) [ethyl(isopropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 8.23-8.25 (bs, 1H), 7.89- m/e 352 1,3-dihydro-2H- 7.92 (m, 2H), 7.45-7.48 (m, 2H), 7.19-7.23 (M + H)⁺ isoindole-2- (m, 2H), 7.15-7.18 (m, 2H), 4.85 (s, 4H), carboxamide 4.27 (p, J = 6.7 Hz, 1H), 3.36 (q, J = 7.0 Hz, 2H), 1.18 (t, J = 6.9 Hz, 3H), 1.11 (d, J = 6.7 Hz, 6H) 265 N-{4-[(3- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (APCI(+)) fluoropyrrolidin-1- Oxide) δ ppm 7.63-7.66 (m, 2H), 7.36-7.41 m/e 354 yl)carbonyl]phenyl}- (m, 2H), 7.33-7.36 (m, 2H), 7.31-7.35 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 5.21-5.48 (m, 1H), 4.79 (s, 4H), 3.53- isoindole-2- 3.79 (m, 4H), 1.98-2.25 (m, 2H) carboxamide 266 N-{4-[(1,3-dihydro- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) 2H-isoindol-2- Oxide) δ ppm 7.59-7.62 (m, 2H), 7.37-7.40 m/e 396 ylcarbonyl)amino]benzoyl}- (m, 2H), 7.31-7.36 (m, 2H), 7.24-7.27 (m, (M + H)⁺ N-isopropyl- 2H), 4.78-4.79 (bs, 4H), 1.00-1.27 (m, 6H) beta-alanine 267 N-{4- ¹H NMR (400 MHz, DMSO-d₆, (ESI(+)) [methyl(propyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 0.82 (t, J = 7.32 Hz, 3H), m/e 338 1,3-dihydro-2H- 1.49-1.62 (m, 2H), 2.92 (s, 3H), 3.27- (M + H)⁺ isoindole-2- 3.34 (m, 2H), 4.78 (s, 4H), 7.23-7.37 (m, 6 carboxamide H), 7.58-7.63 (m, 2H), 8.26 (s, 1H) 268 5,6-dimethoxy-N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.54 (ESI(+)) phenylpropyl)carbamoyl]phenyl}- (s, 1H), 8.29 (t, J = 5.6 Hz, 1H), 7.75-7.78 m/e 460 1,3-dihydro-2H- (m, 2H), 7.61-7.68 (m, 2H), 7.15-7.32 (m, (M + H)⁺ isoindole-2- 5H), 6.95 (s, 2H), 4.69-4.70 (bs, 4H), 3.32 (s, carboxamide 6H), 3.21-3.30 (m, 2H), 2.59-2.68 (m, 2H), 1.76-1.90 (m, 2H) 269 N-(4-{[3-(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) chlorophenoxy)pro- (s, 1H), 8.36 (t, J = 5.6 Hz, 1H), 7.75-7.79 m/e 450 pyl]carbamoyl}phenyl)- (m, 2H), 7.64-7.68 (m, 2H), 7.29-7.39 (m, (M + H)⁺ 1,3-dihydro-2H- 6H), 6.94-6.98 (m, 2H), 4.79 (s, 4H), 4.03 (t, isoindole-2- J = 6.1 Hz, 2H), 3.37-3.44 (m, 2H), 1.97 (p, carboxamide J = 6.5 Hz, 2H) 270 N-(4-{[4- ¹H NMR (500 MHz, DMSO-d₆/Deuterium (ESI(+)) (trifluoromethoxy)phe- Oxide) δ ppm 7.89-7.93 (m, 2H), 7.85-7.89 m/e 442 nyl]carbamoyl}phenyl)- (m, 2H), 7.72-7.75 (m, 2H), 7.33-7.41 (m, (M + H)⁺ 1,3-dihydro-2H- 6H), 4.80-4.82 (bs, 4H) isoindole-2- carboxamide 271 N-{4-[(4-phenyl-1,3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) thiazol-2- Oxide, Temp = 90° C.) δ ppm 8.06-8.09 (m, m/e 441 yl)carbamoyl]phenyl}- 2H), 7.94-7.97 (m, 2H), 7.75-7.78 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.55 (s, 1H), 7.44-7.49 (m, 2H), 7.37-7.41 isoindole-2- (m, 2H), 7.32-7.37 (m, 3H), 4.84 (s, 4H) carboxamide 284 5-bromo-N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.60 (ESI(+)) (propylcarbamoyl)phenyl]- (s, 1H), 8.25 (t, J = 5.6 Hz, 1H), 7.74-7.78 m/e 402 1,3-dihydro- (m, 2H), 7.62-7.67 (m, 2H), 7.59-7.62 (m, (M + H)⁺ 2H-isoindole-2- 1H), 7.50 (dd, J = 8.1, 1.9 Hz, 1H), 7.34 (d, J = carboxamide 8.1 Hz, 1H), 4.70-4.82 (m, 4H), 3.15-3.26 (m, 2H), 1.45-1.61 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 373 5-fluoro-N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) (propylcarbamoyl)phenyl]- (s, 1H), 8.25 (t, J = 5.6 Hz, 1H), 7.74-7.78 m/e 342 1,3-dihydro- (m, 2H), 7.62-7.66 (m, 2H), 7.39 (dd, J = (M + H)⁺ 2H-isoindole-2- 8.4, 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.3 Hz, carboxamide 1H), 7.10-7.19 (m, 1H), 4.74-4.78 (m, 4H), 3.16-3.21 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H); 412 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d₆, (ESI(+)) methoxyethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 3.27 (s, 3H), 3.35-3.49 m/e 340 1,3-dihydro-2H- (m, 4H), 4.79 (s, 4H), 7.25-7.40 (m, 4H), (M + H)⁺ isoindole-2- 7.62-7.69 (m, 2H), 7.74-7.81 (m, 2H), carboxamide 8.31 (t, J = 5.09 Hz, 1H), 8.57 (s, 1H) 413 N-{4-[(5- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) chloropyridin-2- Oxide, Temp = 90° C.) δ ppm 8.37 (d, J = 2.7 m/e 393 yl)carbamoyl]phenyl}- Hz, 1H), 8.16 (d, J = 8.9 Hz, 1H), 7.94-7.97 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 7.89 (dd, J = 8.8, 2.6 Hz, 1H), 7.69- isoindole-2- 7.72 (m, 2H), 7.35-7.38 (m, 2H), 7.30-7.33 carboxamide (m, 2H), 4.81 (s, 4H) 414 N-{4-[(3-hydroxy-4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) methoxyphenyl)carbamoyl]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.85-7.88 (m, m/e 404 1,3-dihydro-2H- 2H), 7.66-7.69 (m, 2H), 7.34-7.39 (m, 2H), (M + H)⁺ isoindole-2- 7.30-7.34 (m, 2H), 7.28-7.30 (m, 1H), 7.09 carboxamide (dd, J = 8.6, 2.5 Hz, 1H), 6.88 (d, J = 8.6 Hz, 1H), 4.81 (s, 4H), 3.77 (s, 3H) 415 N-{4-[(2,4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) dimethoxybenzyl)carbamoyl]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.77-7.79 (m, m/e 432 1,3-dihydro-2H- 2H), 7.61-7.64 (m, 2H), 7.33-7.38 (m, 2H), (M + H)⁺ isoindole-2- 7.28-7.34 (m, 2H), 7.14 (d, J = 8.2 Hz, 1H), carboxamide 6.55 (d, J = 2.4 Hz, 1H), 6.48 (dd, J = 8.2, 2.4 Hz, 1H), 4.79 (s, 4H), 4.38-4.40 (m, 2H), 3.82 (s, 3H), 3.75 (s, 3H) 416 N-(4-{[4-(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) oxopyrrolidin-1- Oxide, Temp = 90° C.) δ ppm 7.78-7.80 (m, m/e 455 yl)benzyl]carbamoyl}phenyl)- 2H), 7.62-7.68 (m, 2H), 7.54-7.56 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.29-7.38 (m, 6H), 4.79 (s, 4H), 4.45-4.47 isoindole-2- (m, 2H), 3.82 (t, J = 7.0 Hz, 2H), 2.45-2.50 carboxamide (m, 2H), 2.04-2.13 (m, 2H) 417 N-(4-{[(1S,2S)-2- ¹H NMR (400 MHz, DMSO-d₆, (ESI(+)) hydroxy-2,3-dihydro- Temp = 90° C.) δ ppm 2.67-2.83 (m, 1H), m/e 414 1H-inden-1- 3.18 (dd, J = 15.47, 7.14 Hz, 1H), 4.34-4.49 (M + H)⁺ yl]carbamoyl}phenyl)- (m, 1H), 4.79 (s, 4H), 5.25-5.34 (m, 2H), 1,3-dihydro-2H- 7.06-7.24 (m, 4H), 7.30-7.42 (m, 4H), isoindole-2- 7.69 (d, J = 8.73 Hz, 2H), 7.87 (d, J = 9.12 Hz, carboxamide 2H), 8.50-8.62 (m, 2H) 418 N-(4-{[(1- ¹H NMR (400 MHz, DMSO-d₆, (ESI(−)) hydroxycyclopropyl) Temp = 90° C.) δ ppm 0.55 (s, 4H), 3.42 (d, m/e 350 methyl]carbamoyl}phenyl)- J = 5.55 Hz, 2H), 4.79 (s, 4H), 5.41 (s, 1H), (M + H)⁺ 1,3-dihydro- 7.28-7.41 (m, 4H), 7.64-7.70 (m, 2H), 2H-isoindole-2- 7.75-7.84 (m, 2H), 8.20 (t, J = 5.75 Hz, 1 carboxamide H), 8.58 (s, 1H) 419 N-{4-[(tetrahydro- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (ESI(−)) 2H-pyran-2- (s, 1H), 8.29 (t, J = 5.8 Hz, 1H), 7.76-7.80 m/e 378 ylmethyl)carbamoyl] (m, 2H), 7.64-7.68 (m, 2H), 7.30-7.39 (m, (M + H)⁺ phenyl}-1,3-dihydro- 4H), 4.78-4.79 (bs, 4H), 3.84-3.90 (m, 1H), 2H-isoindole-2- 3.32-3.47 (m, 2H), 3.21-3.30 (m, 2H), 1.75- carboxamide 1.81 (m, 1H), 1.58-1.65 (m, 1H), 1.33-1.54 (m, 3H), 1.06-1.28 (m, 1H) 420 N-{4-[(tetrahydro- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) 2H-pyran-3- (s, 1H), 8.27 (t, J = 5.8 Hz, 1H), 7.74-7.79 m/e 380 ylmethyl)carbamoyl] (m, 2H), 7.64-7.68 (m, 2H), 7.30-7.39 (m, (M + H)⁺ phenyl}-1,3-dihydro- 4H), 4.78-4.79 (bs, 4H), 3.68-3.80 (m, 2H), 2H-isoindole-2- 3.26-3.36 (m, 1H), 3.06-3.18 (m, 3H), 1.74- carboxamide 1.82 (m, 2H), 1.38-1.68 (m, 2H), 1.15-1.30 (m, 1H) 421 N-{4-[(tetrahydro- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (ESI(+)) 2H-pyran-4- (s, 1H), 8.28 (t, J = 5.8 Hz, 1H), 7.75-7.79 m/e 380 ylmethyl)carbamoyl] (m, 2H), 7.64-7.68 (m, 2H), 7.25-7.43 (m, (M + H)⁺ phenyl}-1,3-dihydro- 4H), 4.79 (s, 4H), 3.81-3.88 (m, 2H), 3.21- 2H-isoindole-2- 3.31 (m, 2H), 3.14 (t, J = 6.3 Hz, 2H), 1.71- carboxamide 1.86 (m, 1H), 1.56-1.63 (m, 2H), 1.07-1.30 (m, 2H) 425 N-{4-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (ESI(+)) benzoylpiperazin-1- (s, 1H), 7.64-7.68 (m, 2H), 7.40-7.50 (m, m/e 455 yl)carbonyl]phenyl}- 5H), 7.29-7.40 (m, 6H), 4.78-4.79 (bs, 4H), (M + H)⁺ 1,3-dihydro-2H- 3.33-3.86 (m, 8H) isoindole-2- carboxamide 434 N-(4-{[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.54 (ESI(+)) (tetrahydrofuran-3- (s, 1H), 7.62-7.66 (m, 2H), 7.28-7.39 (m, m/e 435 ylmethyl)piperazin-1- 6H), 4.78-4.79 (bs, 4H), 3.88-3.95 (m, 1H), (M + H)⁺ yl]carbonyl}phenyl)- 3.68-3.77 (m, 1H), 3.55-3.64 (m, 1H), 3.39- 1,3-dihydro-2H- 3.56 (m, 4H), 2.46-2.56 (m, 2H), 2.35-2.47 isoindole-2- (m, 4H), 1.85-1.99 (m, 1H), 1.66-1.86 (m, carboxamide 2H), 1.39-1.54 (m, 1H) 435 5-fluoro-N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.60 (ESI(+)) ({[(2S)- (s, 1H), 8.33 (t, J = 5.8 Hz, 1H), 7.76-7.80 m/e 384 tetrahydrofuran-2- (m, 2H), 7.63-7.67 (m, 2H), 7.39 (dd, J = (M + H)⁺ ylmethyl]amino}car- 8.4, 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.4 Hz, bonyl)phenyl]-1,3- 1H), 7.15 (td, J = 8.9, 2.5 Hz, 1H), 4.74-4.79 dihydro-2H- (m, 4H), 3.92-4.03 (m, 1H), 3.74-3.82 (m, isoindole-2- 1H), 3.58-3.66 (m, 1H), 3.24-3.34 (m, 2H), carboxamide 1.76-1.96 (m, 3H), 1.52-1.69 (m, 1H) 436 5-fluoro-N-[4-({[(2R)- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.60 (ESI(+)) tetrahydrofuran-2- (s, 1H), 8.33 (t, J = 5.8 Hz, 1H), 7.76-7.80 m/e 384 ylmethyl]amino}carbonyl)phenyl]- (m, 2H), 7.63-7.67 (m, 2H), 7.39 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 8.4, 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.5 Hz, isoindole-2- 1H), 7.15 (td, J = 8.9, 2.5 Hz, 1H), 4.74-4.79 carboxamide (m, 4H), 3.96 (p, J = 6.3 Hz, 1H), 3.74-3.82 (m, 1H), 3.58-3.66 (m, 1H), 3.22-3.34 (m, 2H), 1.74-1.96 (m, 3H), 1.53-1.64 (m, 1H) 438 N-(4-{[4-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.53 (ESI(+)) methoxyethyl)piperazin-1- (s, 1H), 7.62-7.66 (m, 2H), 7.24-7.43 (m, m/e 409 yl]carbonyl}phenyl)- 6H), 4.78 (s, 4H), 3.44 (t, J = 5.8 Hz, 6H), (M + H)⁺ 1,3-dihydro-2H- 3.23 (s, 3H), 2.43 (s, 4H) isoindole-2- carboxamide 439 N-(4-{[(2S)-2-(2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.51 (ESI(+)) hydroxyethyl)piperidin-1- (s, 1H), 7.61-7.65 (m, 2H), 7.25-7.39 (m, m/e 394 yl]carbonyl}phenyl)- 6H), 4.78-4.79 (bs, 4H), 4.36 (t, J = 5.1 Hz, (M + H)⁺ 1,3-dihydro-2H- 1H), 3.46-4.87 (m, 2H), 3.31-3.43 (m, 2H), isoindole-2- 2.78-3.10 (m, 1H), 1.80-1.97 (m, 1H), 1.52- carboxamide 1.76 (m, 6H), 1.26-1.47 (m, 1H) 449 N-[4-({[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (ESI(−)) hydroxy-1-pyridin-2- (s, 1H), 8.53 (ddd, J = 4.8, 1.8, 0.9 Hz, 1H), m/e 401 ylethyl]amino}carbonyl)phenyl]- 8.46 (d, J = 7.8 Hz, 1H), 7.84-7.88 (m, 2H), (M − H)⁻ 1,3-dihydro-2H- 7.75 (td, J = 7.7, 1.8 Hz, 1H), 7.67-7.73 (m, isoindole-2- 2H), 7.29-7.44 (m, 5H), 7.26 (ddd, J = 7.4, carboxamide 4.9, 1.1 Hz, 1H), 5.10-5.17 (m, 1H), 4.88- 4.93 (m, 1H), 4.80 (s, 3H), 3.73-3.88 (m, 2H) 562 N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 11.42 (ESI(+)) (isobutoxycarbamoyl)phenyl]- (s, 1H), 8.60 (s, 1H), 7.67 (s, 4H), 7.41- m/e 354 1,3-dihydro-2H- 7.28 (m, 4H), 4.79 (bs, 4H), 3.65 (d, J = 6.7 (M + H)⁺ isoindole-2- Hz, 2H), 2.02-1.85 (m, 1H), 0.94 (d, J = carboxamide 6.7 Hz, 6H) 567 5-fluoro-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.59 (s, (ESI(+)) [(tetrahydro-2H- 1H), 8.29 (t, J = 5.8 Hz, 1H), 7.81-7.74 (m, m/e 398 pyran-2- 2H), 7.68-7.61 (m, 2H), 7.40 (dd, J = 8.4, (M + H)⁺ ylmethyl)carbamoyl] 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.5 Hz, 1H), phenyl}-1,3-dihydro- 7.15 (td, J = 8.9, 2.5 Hz, 1H), 4.80-4.73 2H-isoindole-2- (m, 3H), 4.05-3.99 (m, 1H), 3.87 (dd, J = carboxamide 11.3, 3.0 Hz, 1H), 3.24 (dd, J = 8.8, 4.0 Hz, 2H), 1.80-1.74 (m, 1H), 1.66-1.56 (m, 1H), 1.57-1.33 (m, 3H), 1.28-1.04 (m, 1H) 568 5-fluoro-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.59 (s, (ESI(+)) [(tetrahydro-2H- 1H), 8.28 (t, J = 5.7 Hz, 1H), 7.76 (d, J = 8.8 m/e 398 pyran-3- Hz, 2H), 7.65 (d, J = 8.8 Hz, 2H), 7.58- (M + H)⁺ ylmethyl)carbamoyl] 7.32 (m, 1H), 7.31-7.06 (m, 2H), 4.76 (d, J = phenyl}-1,3-dihydro- 8.0 Hz, 4H), 3.85-3.62 (m, 2H), 3.23- 2H-isoindole-2- 2.96 (m, 3H), 1.91-1.69 (m, 2H), 1.68- carboxamide 1.35 (m, 2H), 1.35-1.11 (m, 1H) 569 5-fluoro-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.58 (s, (ESI(+)) [(tetrahydro-2H- 1H), 8.28 (t, J = 5.8 Hz, 1H), 7.80-7.73 (m, m/e 398 pyran-4- 2H), 7.68-7.61 (m, 2H), 7.39 (dd, J = 8.4, (M + H)⁺ ylmethyl)carbamoyl] 5.2 Hz, 1H), 7.24 (dd, J = 9.1, 2.5 Hz, 1H), phenyl}-1,3-dihydro- 7.14 (td, J = 8.9, 2.5 Hz, 1H), 4.80-4.72 2H-isoindole-2- (m, 4H), 3.89-3.79 (m, 2H), 3.28-3.20 (m, carboxamide 1H), 3.14 (t, J = 6.3 Hz, 2H), 1.88-1.69 (m, 1H), 1.64-1.54 (m, 2H), 1.28-1.10 (m, 2H) 570 5-fluoro-N-(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, (ESI(+)) {[(1S)-2-hydroxy-1- 1H), 8.49 (d, J = 8.0 Hz, 1H), 7.88-7.80 m/e 420 phenylethyl]carbamoyl}phenyl)- (m, 2H), 7.71-7.64 (m, 2H), 7.44-7.36 (m, (M + H)⁺ 1,3-dihydro-2H- 3H), 7.36-7.27 (m, 2H), 7.28-7.09 (m, isoindole-2- 3H), 5.12-5.01 (m, 1H), 4.90 (t, J = 5.8 Hz, carboxamide 1H), 4.81-4.73 (m, 4H), 3.78-3.59 (m, 2H) 571 5-fluoro-N-(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (s, (ESI(+)) {[(1S)-2-hydroxy-1- 1H), 8.53 (ddd, J = 4.8, 1.8, 0.9 Hz, 1H), m/e 421 (pyridin-2- 8.46 (d, J = 7.8 Hz, 1H), 7.90-7.82 (m, (M + H)⁺ yl)ethyl]carbamoyl}phenyl)- 2H), 7.78-7.71 (m, 1H), 7.69 (t, J = 5.5 Hz, 1,3-dihydro- 2H), 7.44-7.36 (m, 2H), 7.30-7.09 (m, 2H-isoindole-2- 3H), 5.19-5.08 (m, 1H), 4.90 (t, J = 5.9 Hz, carboxamide 1H), 4.87-4.72 (m, 4H), 3.89-3.72 (m, 2H);) 572 5-fluoro-N-(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.59 (s, (ESI(+)) {[(2S)-1-hydroxy-4- 1H), 7.84-7.75 (m, 3H), 7.68-7.61 (m, m/e 400 methylpentan-2- 2H), 7.40 (dd, J = 8.4, 5.2 Hz, 1H), 7.24 (dd, (M + H)⁺ yl]carbamoyl}phenyl)- J = 9.1, 2.5 Hz, 1H), 7.15 (td, J = 8.9, 2.5 1,3-dihydro-2H- Hz, 1H), 4.80-4.73 (m, 4H), 4.65 (t, J = 5.7 isoindole-2- Hz, 1H), 4.10-3.97 (m, 1H), 3.49-3.35 carboxamide (m, 1H), 1.74-1.54 (m, 1H), 1.52-1.31 (m, 2H), 0.88 (t, J = 6.8 Hz, 6H) 585 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.58 (ESI(+)) hydroxy-4- (s, 1H), 7.90 (d, J = 8.3 Hz, 1H), 7.79 (m, m/e 400 (methylthio)butan-2- 2H), 7.67 (m, 2H), 7.40-7.29 (m, 4H), 4.79 (M + H)⁺ yl]carbamoyl}phenyl)- (s, 4H), 4.73 (m, 1H), 4.03 (m, 1H), 3.47 (m, 1,3-dihydro-2H- 1H), 3.58 (m, 1H), 2.60-2.40 (m, 2H), 2.04 isoindole-2- (s, 3H), 1.90 (m, 1H), 1.74 (m, 1H) carboxamide 586 N-(4-{[(2S,3S)-1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) hydroxy-3- (s, 1H), 7.80 (m, 3H), 7.66 (m, 2H), 7.34 (m, m/e 382 methylpentan-2- 4H), 4.79 (bs, 4H), 4.52 (t, J = 5.5 Hz, 1H), (M + H)⁺ yl]carbamoyl}phenyl)- 3.84 (m, 1H), 3.53 (m, 2H), 1.69 (m, 1H), 1,3-dihydro-2H- 1.49 (m, 1H), 1.10 (m, 1H), 0.91-0.81 (m, 6H) isoindole-2- carboxamide 587 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) hydroxypropan-2- (s, 1H), 7.89 (d, J = 8.0 Hz, 1H), 7.78 (m, m/e 340 yl]carbamoyl}phenyl)- 2H), 7.66 (m, 2H), 7.40-7.29 (m, 4H), 4.79 (M + H)⁺ 1,3-dihydro-2H- (bs, 4H), 4.70 (t, J = 5.7 Hz, 1H), 4.00 (m, isoindole-2- 1H), 3.46 (dt, J = 10.8, 3.33 (m, 1H), 5.4 Hz, carboxamide 1H), 1.13 (d, J = 6.7 Hz, 3H) 588 N-(4-{[(2S,3R)-1,3- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) dihydroxybutan-2- (bs, 1H), 7.78 (m, 3H), 7.67 (m, 2H), 7.40- m/e 370 yl]carbamoyl}phenyl)- 7.29 (m, 4H), 4.79 (bs, 4H), 4.67 (d, J = 5.2 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 4.52 (m, 1H), 3.90-3.72 (m, 2H), isoindole-2- 3.63 (m, 2H), 1.08 (d, J = 6.12 Hz, 3H) carboxamide 589 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) hydroxyhexan-2- (s, 1H), 7.80 (m, 3H), 7.66 (m, 2H), 7.40- m/e 382 yl]carbamoyl}phenyl)- 7.29 (m, 4H), 4.79 (bs, 4H), 4.65 (t, J = 5.7 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 3.93 (m, 1H), 3.44 (dt, J = 10.8, 5.4 isoindole-2- Hz, 1H), 3.32 (m, 1H), 1.63 (m, 1H), 1.44 carboxamide (m, 1H), 1.28 (m, 4H), 0.86 (t, J = 6.3 Hz, 3H) 590 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) hydroxypentan-2- (s, 1H), 7.80 (m, 3H), 7.66 (m, 2H), 7.40- m/e 368 yl]carbamoyl}phenyl)- 7.29 (m, 4H), 4.79 (bs, 4H), 4.64 (t, J = 5.7 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 3.95 (m, 1H), 3.44 (dt, J = 10.8, 5.4 isoindole-2- Hz, 1H), 3.32 (m, 1H), 1.58 (m, 1H), 1.50- carboxamide 1.22 (m, 3H), 0.88 (t, J = 7.3 Hz, 3H) 591 N-(4-{[(1S,2S)-2- - ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) hydroxycyclopentyl] (s, 1H), 8.03 (m, 1H), 7.78 (m, 2H), 7.66 (m, m/e 366 carbamoyl}phenyl)- 2H), 7.40-7.29 (m, 4H), 4.81 (bs, 4H), 4.75 (M + H)⁺ 1,3-dihydro-2H- (t, J = 5.7 Hz, 1H), 4.98 (m, 2H), 1.99 (m, isoindole-2- 1H), 1.86 (m, 1H), 1.65 (m, 2H), 1.47 (m, carboxamide 2H) 592 N-(4-{[(1S,2R)-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) hydroxycyclopentyl] (s, 1H), 7.80 (m, 2H), 7.65 (m, 3H), 7.40- m/e 366 carbamoyl}phenyl)- 7.28 (m, 4H), 4.79 (bs, 4H), 4.71 (d, J = 3.6 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 4.04 (m, 2H), 1.88-1.44 (m, 6H) isoindole-2- carboxamide 593 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.57 (ESI(+)) cyclohexyl-3- (s, 1H), 7.81 (m, 3H), 7.67 (m, 2H), 7.43- m/e 422 hydroxypropan-2- 7.26 (m, 4H), 4.79 (s, 4H), 4.64 (t, J = 5.7 (M + H)⁺ yl]carbamoyl}phenyl)- Hz, 1H), 4.06 (m, 1H), 3.42 (m, 1H), 3.30 1,3-dihydro-2H- (m, 1H), 1.80 (d, J = 12.6 Hz, 1H), 1.62 (m, isoindole-2- 4H), 1.43 (m, 2H), 1.32 (m, 1H), 1.14 (m, carboxamide 3H), 0.95 (m, 1H), 0.83 (m, 1H) 594 N-[4-({(2R)-1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) hydroxy-3-[(4- (s, 1H), 7.98 (d, J = 8.2 Hz, 1H), 7.79 (m, m/e 476 methylbenzyl)thio]propan-2- 2H), 7.68 (m, 2H), 7.40-7.28 (m, 4H), 7.20 (M + H)⁺ yl}carbamoyl)phenyl]- (m, 2H), 7.10 (m, 2H), 4.80 (m, 5H), 4.13 1,3-dihydro-2H- (m, 1H), 3.71 (s, 2H), 3.55 (m, 1H), 3.44 (m, isoindole-2- 1H), 2.70 (dd, J = 13.3, 5.7 Hz, 1H), 2.55 carboxamide (m, 1H), 2.27 (s, 3H) 595 N-(4-{[(1S)-1-(4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.59 (ESI(+)) tert-butylphenyl)-2- (s, 1H), 8.45 (d, J = 8.0 Hz, 1H), 7.83 (m, m/e 458 hydroxyethyl]carbamoyl}phenyl)- 2H), 7.68 (m, 2H), 7.40-7.27 (m, 8H), 5.03 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 4.87 (t, J = 5.8 Hz, 1H), 4.79 (bs, isoindole-2- 4H), 3.67 (m, 2H), 1.26 (s, 9H) carboxamide 597 5-methoxy-N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.53 (ESI(+)) (propylcarbamoyl)phenyl]- (s, 1H), 8.24 (m, 1H), 7.80-7.72 (m, 2H), m/e 354 1,3-dihydro- 7.67-7.61 (m, 2H), 7.26 (d, J = 8.3 Hz, (M + H)⁺ 2H-isoindole-2- 1H), 6.98-6.91 (m, 1H), 6.88 (dd, J = 8.3, carboxamide 2.4 Hz, 1H), 4.72 (m, 4H), 3.77 (s, 3H), 3.25- 3.14 (m, 2H), 1.60-1.44 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 598 5-methyl-N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.54 (ESI(+)) (propylcarbamoyl)phenyl]- (s, 1H), 8.24 (m, 1H), 7.80-7.72 (m, 2H), m/e 338 1,3-dihydro- 7.69-7.61 (m, 2H), 7.24 (d, J = 7.7 Hz, (M + H)⁺ 2H-isoindole-2- 1H), 7.17 (bs, 1H), 7.16-7.09 (m, 1H), 4.73 carboxamide (bs, 4H), 3.23-3.14 (m, 2H), 2.33 (s, 3H), 1.60-1.44 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 716 N-(4-{[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, (ESI(+)) methylpyrrolidin-3- 1H), 8.40 (t, J = 5.7 Hz, 1H), 7.81-7.73 (m, m/e 379 yl)methyl]carbamoyl}phenyl)- 2H), 7.71-7.63 (m, 2H), 7.41-7.28 (m, (M + H)⁺ 1,3-dihydro-2H- 6H), 5.83 (dd, J = 19.3, 15.2 Hz, 1H), 4.79 isoindole-2- (bs, 4H), 3.30-3.21 (m, 1H), 3.06-2.93 carboxamide (m, 1H), 2.89-2.69 (m, 1H), 2.60 (dd, J = 17.2, 7.4 Hz, 1H), 2.32 (s, 3H), 2.04-1.85 (m, 1H), 1.58 (tt, J = 13.9, 6.9 Hz, 1H) 719 N-(4-{[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.57 (s, (ESI(+)) methylpiperidin-4- 1H), 8.27 (t, J = 5.8 Hz, 1H), 7.80-7.73 (m, m/e 393 yl)methyl]carbamoyl}phenyl)- 2H), 7.69-7.62 (m, 2H), 7.41-7.28 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.35-3.27 (m, 2H), 3.13 (t, J = 6.2 Hz, isoindole-2- 2H), 3.03-2.93 (m, 1H), 2.86-2.77 (m, carboxamide 2H), 2.20 (s, 3H), 2.17 (s, 1H), 2.00-1.82 (m, 2H), 1.70-1.45 (m, 3H), 1.28-1.11 (m, 2H) 781 N-(4-{[(1,1- ¹H NMR (300 MHz, DMSO DMSO-d₆) δ (ESI(+)) dioxidotetrahydrothiophen-3- 8.58 (s, 1H), 8.44 (t, J = 5.8 Hz, 1H), 7.81- m/e 414 yl)methyl]carbamoyl}phenyl)- 7.74 (m, 2H), 7.71-7.64 (m, 2H), 7.41- (M + H)⁺ 1,3-dihydro-2H- 7.28 (m, 4H), 4.79 (s, 4H), 3.41-3.31 (m, isoindole-2- 2H), 3.30 (s, 2H), 3.11-2.81 (m, 2H), 2.74- carboxamide 2.59 (m, 1H), 2.30-2.15 (m, 1H), 1.94- 1.76 (m, 1H) 782 N-(4-{[(2,2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.58 (s, (ESI(+)) dimethyl-1,3- 1H), 8.38 (t, J = 5.8 Hz, 1H), 8.01-7.89 (m, m/e 396 dioxolan-4- 1H), 7.78 (d, J = 8.9 Hz, 2H), 7.67 (d, J = (M + H)⁺ yl)methyl]carbamoyl}phenyl)- 8.8 Hz, 2H), 7.44-7.24 (m, 4H), 4.79 (s, 1,3-dihydro-2H- 4H), 4.20 (p, J = 5.9 Hz, 1H), 3.98 (dd, J = isoindole-2- 8.3, 6.2 Hz, 1H), 3.71 (dd, J = 8.3, 5.8 Hz, carboxamide 1H), 3.50-3.20 (m, 1H), 1.35 (s, 3H), 1.26 (s, 3H) 783 N-(4-{[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (d, J = (ESI(+)) methoxy-1- 8.2 Hz, 2H), 7.87-7.79 (m, 2H), 7.70 (s, m/e 416 phenylethyl]carbamoyl}phenyl)- 1H), 7.67 (s, 1H), 7.46-7.20 (m, 9H), 5.27 (M + H)⁺ 1,3-dihydro-2H- (td, J = 8.4, 5.4 Hz, 1H), 4.79 (s, 4H), 3.70 isoindole-2- (dd, J = 10.0, 8.6 Hz, 1H), 3.55 (dd, J = 10.0, carboxamide 5.5 Hz, 1H), 3.30 (d, J = 2.9 Hz, 3H) 784 N-[4-({[(4S)-2,2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.58 (s, (ESI(+)) dimethyl-1,3- 1H), 8.39 (t, J = 5.8 Hz, 1H), 7.81-7.74 (m, m/e 396 dioxolan-4- 2H), 7.70-7.63 (m, 2H), 7.41-7.28 (m, (M + H)⁺ yl]methyl}carbamoyl)phenyl]- 4H), 4.79 (s, 4H), 4.20 (p, J = 5.9 Hz, 1H), 1,3-dihydro-2H- 3.98 (dd, J = 8.3, 6.2 Hz, 1H), 3.71 (dd, J = isoindole-2- 8.3, 5.8 Hz, 1H), 3.30 (s, 1H), 1.35 (s, 3H), carboxamide 1.26 (s, 3H) 785 N-[4-({[(4R)-2,2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.58 (s, (ESI(+)) dimethyl-1,3- 1H), 8.39 (t, J = 5.8 Hz, 1H), 7.81-7.74 (m, m/e 396 dioxolan-4- 2H), 7.70-7.63 (m, 2H), 7.43-7.27 (m, (M + H)⁺ yl]methyl}carbamoyl)phenyl]- 4H), 4.79 (s, 4H), 4.20 (p, J = 5.9 Hz, 1H), 1,3-dihydro-2H- 3.98 (dd, J = 8.3, 6.2 Hz, 1H), 3.71 (dd, J = isoindole-2- 8.3, 5.8 Hz, 1H), 3.38 (ddd, J = 14.9, 12.8, carboxamide 5.8 Hz, 1H), 1.35 (s, 3H), 1.26 (s, 3H) 786 N-[4-({[3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, (ESI(+)) (hydroxymethyl)oxetan-3- 1H), 8.43 (t, J = 6.1 Hz, 1H), 7.83-7.76 (m, m/e 382 yl]methyl}carbamoyl)phenyl]- 2H), 7.72-7.65 (m, 2H), 7.41-7.28 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 4.89 (t, J = 5.6 Hz, 1H), 4.79 (s, 4H), isoindole-2- 4.40 (d, J = 5.9 Hz, 2H), 4.29 (d, J = 5.8 Hz, carboxamide 2H), 3.58 (d, J = 5.6 Hz, 2H), 3.51 (d, J = 6.0 Hz, 2H) 790 N-{4-[(2R)-butan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ylcarbamoyl]phenyl}- δ 7.81-7.71 (m, 2H), 7.71-7.48 (m, 2H), m/e 338 1,3-dihydro-2H- 7.44-7.23 (m, 4H), 4.79 (s, 4H), 3.92 (h, J = (M + H)⁺ isoindole-2- 6.7 Hz, 1H), 1.62-1.44 (m, 2H), 1.15 (d, carboxamide J = 6.6 Hz, 3H), 0.88 (t, J = 7.4 Hz, 3H) 802 N-(4-{[(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.59 (s, (ESI(+)) methyloxetan-3- 1H), 8.43 (t, J = 6.1 Hz, 1H), 7.83-7.76 (m, m/e 366 yl)methyl]carbamoyl}phenyl)- 2H), 7.71-7.65 (m, 2H), 7.41-7.28 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 4.79 (s, 4H), 4.48 (d, J = 5.7 Hz, 2H), isoindole-2- 4.20 (d, J = 5.7 Hz, 2H), 3.44 (d, J = 6.0 Hz, carboxamide 2H), 1.25 (s, 3H) 809 5-cyano-N-{4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) [(cyclopentylmethyl) Temp = 90° C.) δ ppm 7.79 (s, 1H) 7.70-7.77 m/e 389 carbamoyl]phenyl}- (m, 3H) 7.60-7.63 (m, 1H) 7.58-7.60 (m, (M + H)⁺ 1,3-dihydro-2H- 1H) 7.56 (d, J = 7.93 Hz, 1H) 4.85 (d, isoindole-2- J = 8.24 Hz, 4H) 3.21 (d, J = 7.02 Hz, 2H) carboxamide 2.08-2.25 (m, 1H) 1.43-1.76 (m, 6H) 1.19-1.35 (m, 2H) 810 5-cyano-N-{4-[(1,3- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) thiazol-5- Temp = 90° C.) δ ppm 7.74-7.81 (m, 4H) m/e 404 ylmethyl)carbamoyl] 7.72 (dd, J = 7.93, 1.53 Hz, 1H) 7.61-7.65 (M + H)⁺ phenyl}-1,3-dihydro- (m, 2H) 7.56 (d, J = 7.93 Hz, 2H) 4.85 (d, 2H-isoindole-2- J = 9.77 Hz, 4H) 4.68 (s, 2H) carboxamide 811 5-cyano-N-(4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) {[(1R)-3-hydroxy-1- Temp = 90° C.) δ ppm 7.75-7.81 (m, 3H) m/e 441 phenylpropyl]carbamoyl}phenyl)- 7.70-7.73 (m, 1H) 7.60-7.64 (m, 2H) (M + H)⁺ 1,3-dihydro-2H- 7.56 (d, J = 7.93 Hz, 1H) 7.37-7.43 (m, 2H) isoindole-2- 7.28-7.35 (m, 2H) 7.17-7.25 (m, 1H) carboxamide 5.11-5.22 (m, 1H) 4.85 (d, J = 8.24 Hz, 4H) 3.44-3.52 (m, 2H) 1.91-2.12 (m, 2H) 812 5-cyano-N-(4-{[2- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) hydroxy-1-(4- Temp = 90° C.) δ ppm 7.77-7.82 (m, 3 H) m/e 441 methylphenyl)ethyl]carbamoyl}phenyl)- 7.72 (dd, J = 7.93, 1.53 Hz, 1H) 7.59-7.65 (M + H)⁺ 1,3-dihydro-2H- (m, 2H) 7.56 (d, J = 7.93 Hz, 1H) 7.27 (d, isoindole-2- J = 8.24 Hz, 2H) 7.12 (d, J = 7.93 Hz, 2H) carboxamide 5.00-5.07 (m, 1H) 4.85 (d, J = 8.24 Hz, 4H) 3.67-3.78 (m, 2H) 2.27 (s, 3H) 813 5-cyano-N-{4-[(1,3- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) dihydroxypropan-2- Temp = 90° C.) δ ppm 7.86-8.00 (m, 1H) m/e 381 yl)carbamoyl]phenyl}- 7.67-7.81 (m, 4H) 7.53-7.65 (m, 2H) (M + H)⁺ 1,3-dihydro-2H- 4.85 (d, J = 7.02 Hz, 4H) 4.33-4.52 (m, 1H) isoindole-2- 3.93-4.02 (m, 1H) 3.59-3.84 (m, 1H) carboxamide 3.58 (d, J = 5.80 Hz, 2H) 814 5-cyano-N-(4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) {[(2R)-2- Temp = 90° C.) δ ppm 7.68-7.84 (m, 4H) m/e 365 hydroxypropyl]carbamoyl}phenyl)- 7.54-7.64 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ 1,3-dihydro-2H- 3.77-3.88 (m, 1H) 3.15-3.26 (m, 2H) isoindole-2- 1.10 (d, J = 6.10 Hz, 3H) carboxamide 815 5-cyano-N-{4-[(2- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) hydroxy-2- Temp = 90° C.) δ ppm 7.69-7.81 (m, 4H) m/e 379 methylpropyl)carbamoyl]phenyl}- 7.54-7.65 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ 1,3-dihydro-2H- 3.28 (s, 2H) 1.14 (s, 6H) isoindole-2- carboxamide 816 5-cyano-N-(4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) {[(2R)-1-hydroxy-3- Temp = 90° C.) δ ppm 7.69-7.81 (m, 4H) m/e 393 methylbutan-2- 7.55-7.64 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ yl]carbamoyl}phenyl)- 3.76-3.84 (m, 1H) 3.56 (d, J = 5.19 Hz, 2H) 1,3-dihydro-2H- 1.87-2.00 (m, 1H) 0.92 (dd, J = 11.75, 6.87 isoindole-2- Hz, 6H) carboxamide 817 5-cyano-N-(4-{[(2S)- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) tetrahydrofuran-2- Temp = 90° C.) δ ppm 7.69-7.81 (m, 4H) m/e 391 ylmethyl]carbamoyl} 7.54-7.63 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ phenyl)-1,3-dihydro- 3.95-4.05 (m, 1H) 3.75-3.84 (m, 1H) 2H-isoindole-2- 3.60-3.68 (m, 1H) 3.34 (d, J = 5.80 Hz, 2H) carboxamide 1.75-1.98 (m, 3H) 1.54-1.66 (m, 1H) 818 5-cyano-N-(4-{[2-(4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) methylpiperazin-1- Temp = 90° C.) δ ppm 7.70-7.81 (m, 4H) m/e 433 yl)ethyl]carbamoyl}phenyl)- 7.60-7.66 (m, H) 7.57 (d, J = 7.93 Hz, 1H) (M + H)⁺ 1,3-dihydro- 4.85 (d, J = 8.85 Hz, 4H) 3.50 (t, J = 6.41 Hz, 2H-isoindole-2- 2H) 3.22-3.26 (m, 4H) 3.04 (d, J = 4.88 Hz, carboxamide 4H) 2.90 (t, J = 6.41 Hz, 2H) 2.78 (s, 3H) 819 5-cyano-N-(4-{[(1S) ¹H NMR (400 MHz, DMSO-D₂O_(,) Temp = 90° (ESI(+)) 2-hydroxy-1- C.) δ ppm 7.78-7.85 (m, 3H) 7.70-7.74 m/e 427 phenylethyl]carbamoyl}phenyl)- (m, 1H) 7.60-7.66 (m, 2H) 7.56 (d, J = 8.24 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H) 7.38-7.43 (m, 2H) 7.28-7.34 (m, isoindole-2- 2H) 7.19-7.26 (m, 1H) 5.03-5.13 (m, 1 carboxamide H) 4.85 (d, J = 8.24 Hz, 4H) 3.68-3.79 (m, 2H) 820 5-cyano-N-{4-[(4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) hydroxybutyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 7.79 (s, 1H) 7.70-7.76 m/e 377 1,3-dihydro-2H- (m, 3H) 7.58-7.64 (m, 2H) 7.56 (d, J = 8.24 (M + H)⁺ isoindole-2- Hz, 1H) 4.85 (d, J = 8.24 Hz, 4H) 4.44 (t, carboxamide J = 6.41 Hz, 1H) 3.45 (t, J = 6.41 Hz, 1H) 3.27-3.34 (m, 2H) 1.46-1.81 (m, 4H) 821 5-cyano-N-(4-{[(2S)-2- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) hydroxypropyl]carbamoyl}phenyl)- Temp = 90° C.) δ ppm 7.69-7.82 (m, 4H) m/e 365 1,3-dihydro-2H-isoindole-2- 7.53-7.64 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ carboxamide 3.79-3.87 (m, 1H) 3.17-3.26 (m, 2H) 1.10 (d, J = 6.10 Hz, 3H) 822 5-cyano-N-{4-[(3- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) furylmethyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 7.79 (s, 1H) 7.74-7.78 m/e 387 1,3-dihydro-2H- (m, 2H) 7.72 (d, J = 7.93 Hz, 1H) 7.59-7.65 (M + H)⁺ isoindole-2- (m, 2H) 7.54-7.58 (m, 1H) 7.50-7.53 (m, carboxamide 1H) 7.25 (d, J = 8.54 Hz, 1H) 6.46 (s, 1H) 4.85 (d, J = 8.85 Hz, 4H) 4.31 (s, 2H) 823 5-cyano-N-{4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) [(tetrahydrofuran-2- Temp = 90° C.) δ ppm 7.70-7.81 (m, 4H) m/e 391 ylmethyl)carbamoyl] 7.55-7.64 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ phenyl}-1,3-dihydro- 3.95-4.04 (m, 1H) 3.75-3.83 (m, 1H) 2H-isoindole-2- 3.61-3.68 (m, 1H) 3.34 (d, J = 5.80 Hz, 2H) carboxamide 1.75-1.98 (m, 3H) 1.54-1.65 (m, 1H) 824 5-cyano-N-(4-{[4-(2- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) furoyl)piperazin-1- Temp = 90° C.) δ ppm 7.79 (s, 1H) 7.73-7.75 m/e 470 yl]carbonyl}phenyl)- (m, 1H) 7.71 (d, J = 1.53 Hz, 1H) 7.60-7.65 (M + H)⁺ 1,3-dihydro-2H- (m, 2H) 7.57 (d, J = 8.54 Hz, 1H) 7.34-7.40 isoindole-2- (m, 2H) 7.00 (d, J = 2.75 Hz, 1H) 6.59 (dd, carboxamide J = 3.51, 1.68 Hz, 1H) 4.85 (d, J = 8.54 Hz, 4 H) 3.71-3.77 (m, 4H) 3.54-3.65 (m, 4H) 825 5-cyano-N-(4-{[4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) (tetrahydrofuran-2- Temp = 90° C.) δ ppm 7.79 (s, 1H) 7.72 (dd, m/e 474 ylcarbonyl)piperazin-1- J = 7.93, 1.53 Hz, 1H) 7.59-7.64 (m, 2H) (M + H)⁺ yl]carbonyl}phenyl)- 7.57 (d, J = 7.93 Hz, 1H) 7.33-7.37 (m, 2H) 1,3-dihydro-2H- 4.85 (d, J = 8.24 Hz, 4H) 4.64 (dd, J = 7.48, isoindole-2- 5.95 Hz, 1H) 3.71-3.86 (m, 2H) 3.48- carboxamide 3.61 (m, 8H) 1.96-2.14 (m, 2H) 1.75- 1.94 (m, 2H) 826 5-cyano-N-(4-{[3- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) (piperidin-1- Temp = 90° C.) δ ppm 7.70-7.81 (m, 4H) m/e 432 yl)propyl]carbamoyl}phenyl)- 7.61-7.66 (m, 2H) 7.57 (d, J = 7.93 Hz, 1H) (M + H)⁺ 1,3-dihydro-2H- 4.85 (d, J = 8.24 Hz, 4H) 3.36 (t, J = 6.71 Hz, isoindole-2- 4H) 3.02-3.13 (m, 2H) 2.90 (s, 2H) 1.90- carboxamide 2.18 (m, 2H) 1.81 (d, J = 84.53 Hz, 6H) 827 5-cyano-N-(4-{[(2R)- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) tetrahydrofuran-2- Temp = 90° C.) δ ppm 7.70-7.81 (m, 4H) m/e 391 ylmethyl]carbamoyl} 7.55-7.64 (m, 3H) 4.85 (d, J = 8.54 Hz, 4H) (M + H)⁺ phenyl)-1,3-dihydro- 3.96-4.04 (m, 1H) 3.76-3.85 (m, 1H) 2H-isoindole-2- 3.61-3.68 (m, 1H) 3.34 (d, J = 5.80 Hz, 2H) carboxamide 1.75-1.98 (m, 3H) 1.54-1.67 (m, 1H) 828 5-cyano-N-(4-{[4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) (ethylsulfonyl)piperazin-1- Temp = 90° C.) δ ppm 7.79 (s, 1H) 7.72 (dd, m/e 468 yl]carbonyl}phenyl)- J = 7.93, 1.53 Hz, 1H) 7.59-7.64 (m, 2H) (M + H)⁺ 1,3-dihydro-2H- 7.57 (d, J = 7.63 Hz, 1H) 7.32-7.37 (m, 2H) isoindole-2- 4.85 (d, J = 8.24 Hz, 4H) 3.56-3.61 (m, 4H) carboxamide 3.27 (s, 4H) 3.07 (q, J = 7.32 Hz, 2H) 1.24 (t, J = 7.32 Hz, 3H) 829 5-cyano-N-{4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) [(tetrahydrofuran-3- Temp = 90° C.) δ ppm 7.79 (s, 1H) 7.72-7.77 m/e 391 ylmethyl)carbamoyl] (m, 2H) 7.71 (d, J = 1.22 Hz, 1H) 7.59-7.64 (M + H)⁺ phenyl}-1,3-dihydro- (m, 2H) 7.57 (d, J = 7.93 Hz, 1H) 4.85 (d, 2H-isoindole-2- J = 8.24 Hz, 4H) 3.69-3.80 (m, 2H) 3.60- carboxamide 3.67 (m, 1H) 3.47 (dd, J = 8.54, 5.49 Hz, 1 H) 3.28-3.30 (m, J = 3.36 Hz, 2H) 2.45- 2.50 (m, 1H) 1.90-2.01 (m, 1H) 1.58- 1.68 (m, 1H) 830 5-cyano-N-(4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) {[(1R)-2-hydroxy-1- Temp = 90° C.) δ ppm 7.81-7.83 (m, 1H) m/e 427 phenylethyl]carbamoyl}phenyl)- 7.78-7.80 (m, 2H) 7.72 (dd, J = 7.93, 1.53 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H) 7.61-7.64 (m, 2H) 7.57 (d, J = 8.54 isoindole-2- Hz, 1H) 7.39 (d, J = 7.63 Hz, 2H) 7.28-7.34 carboxamide (m, 2H) 7.20-7.25 (m, 1H) 5.05-5.11 (m, 1 H) 4.83-4.88 (m, 4H) 3.69-3.79 (m, 2H) 831 5-cyano-N-(4-{[(2S)- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) 1-hydroxybutan-2- Temp = 90° C.) δ ppm 7.67-7.90 (m, 4H) m/e 379 yl]carbamoyl}phenyl)- 7.52-7.65 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ 1,3-dihydro-2H- 3.79-3.93 (m, 1H) 3.41-3.55 (m, 2H) isoindole-2- 1.41-1.85 (m, 2H) 0.90 (t, J = 7.48 Hz, 3H) carboxamide 832 5-cyano-N-{4-[(2,3- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) dihydroxypropyl)carbamoyl]phenyl}- Temp = 90° C.) δ ppm 7.70-7.81 (m, 4H) m/e 381 1,3-dihydro-2H- 7.54-7.65 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ isoindole-2- 3.62-3.73 (m, 1H) 3.38-3.45 (m, 3H) carboxamide 3.29 (d, J = 6.41 Hz, 1H) 833 5-cyano-N-{4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) [(tetrahydro-2H- Temp = 90° C.) δ ppm 7.69-7.84 (m, 4H) m/e 405 pyran-4- 7.52-7.64 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ ylmethyl)carbamoyl] 3.80-3.89 (m, 2H) 3.28-3.35 (m, 2H) phenyl}-1,3-dihydro- 3.19 (d, J = 7.02 Hz, 2H) 1.76-1.91 (m, 1H) 2H-isoindole-2- 1.61 (dd, J = 12.82, 1.83 Hz, 2H) 1.17-1.32 carboxamide (m, 2H) 834 5-cyano-N-(4-{[2- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) hydroxy-1-(pyridin-2- Temp = 90° C.) δ ppm 8.60 (d, J = 4.27 Hz, 1 m/e 428 yl)ethyl]carbamoyl}phenyl)- H) 7.96-8.04 (m, 1H) 7.77-7.86 (m, 3H) (M + H)⁺ 1,3-dihydro- 7.73 (d, J = 7.93 Hz, 1H) 7.61-7.68 (m, 3H) 2H-isoindole-2- 7.57 (d, J = 7.93 Hz, 1H) 7.45-7.51 (m, 1H) carboxamide 5.21 (t, J = 5.95 Hz, 1H) 4.86 (d, J = 8.24 Hz, 4H) 3.89 (d, J = 5.80 Hz, 2 H) 835 5-cyano-N-{4-[(1- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) hydroxy-4- Temp = 90° C.) δ ppm 7.68-7.82 (m, 4H) m/e 407 methylpentan-2- 7.52-7.64 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ yl)carbamoyl]phenyl}- 4.01-4.09 (m, 1H) 3.38-3.52 (m, 2H) 1,3-dihydro-2H- 1.59-1.75 (m, 1H) 1.37-1.55 (m, 2H) isoindole-2- 0.86-0.93 (m, 6H) carboxamide 836 5-cyano-N-(4-{[(1- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) methylpyrrolidin-3- Temp = 90° C.) δ ppm 7.70-7.82 (m, 4H) m/e 404 yl)methyl]carbamoyl}phenyl)- 7.59-7.67 (m, 2H) 7.57 (d, J = 7.63 Hz, 1H) (M + H)⁺ 1,3-dihydro-2H- 4.82-4.89 (m, 4H) 3.41-3.82 (m, 2H) isoindole-2- 3.35-3.41 (m, 2H) 2.94-3.21 (m, 2H) carboxamide 2.85 (s, 3H) 2.60-2.75 (m, 1H) 1.61-2.34 (m, 2H) 837 5-cyano-N-(4-{[(1- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) methylpiperidin-4- Temp = 90° C.) δ ppm 7.67-7.83 (m, 4H) m/e 418 yl)methyl]carbamoyl}phenyl)- 7.54-7.65 (m, 3H) 4.85 (d, J = 8.24 Hz, 4H) (M + H)⁺ 1,3-dihydro-2H- 3.36-3.52 (m, 2H) 3.18-3.25 (m, 2H) isoindole-2- 2.92 (s, 2H) 2.76 (s, 3H) 1.89 (m, 3H) 1.29- carboxamide 1.54 (m, 2H) 838 5-cyano-N-{4- ¹H NMR (400 MHz, DMSO-D₂O_(,) (ESI(+)) [(tetrahydro-2H- Temp = 90° C.) δ ppm 7.68-7.82 (m, 4H) m/e 405 pyran-3- 7.52-7.65 (m, 3H) 4.85 (d, J = 8.54 Hz, 4H) (M + H)⁺ ylmethyl)carbamoyl] 3.65-3.82 (m, 2H) 3.29-3.40 (m, 1H) phenyl}-1,3-dihydro- 3.09-3.20 (m, 3H) 1.73-1.92 (m, 2H) 2H-isoindole-2- 1.40-1.69 (m, 2H) 1.20-1.35 (m, 1H) carboxamide 717 N-{4-[(pyrrolidin-3- ¹H NMR (300 MHz, DMSO-d₆) δ 9.07 (bs, (ESI(+)) ylmethyl)carbamoyl] 1H), 8.64 (s, 1H), 8.51 (t, J = 5.8 Hz, 1H), m/e 340 phenyl}-1,3-dihydro- 7.83-7.75 (m, 1H), 7.73-7.65 (m, 2H), (M + H)⁺ 2H-isoindole-2- 7.42-7.28 (m, 3H), 4.86 (bs, 2H), 4.79 (s, carboxamide 4H), 3.75-3.64 (m, 1H), 3.53-3.43 (m, 1H), 3.40-3.16 (m, 3H), 3.10 (dt, J = 13.6, 7.7 Hz, 1H), 2.98-2.83 (m, 1H), 2.07-1.92 (m, 1H), 1.84-1.46 (m, 1H) 840 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.67- (ESI(+)) diazaspiro[3.3]hept-2- 7.61 (m, 2H), 7.57-7.51 (m, 2H), 7.40- m/e 363 ylcarbonyl)phenyl]- 7.26 (m, 4H), 4.79 (s, 4H), 4.36 (bs, 4H), (M + H)⁺ 1,3-dihydro-2H- 4.20 (s, 4H) isoindole-2- carboxamide 841 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.70- (ESI(+)) diazaspiro[3.4]oct-6- 7.56 (m, 2H), 7.48-7.42 (m, 2H), 7.38- m/e 377 ylcarbonyl)phenyl]- 7.29 (m, 4H), 4.79 (s, 4H), 3.99 (q, J = 10.6 (M + H)⁺ 1,3-dihydro-2H- Hz, 4H), 3.74 (s, 2H), 3.52 (t, J = 7.0 Hz, isoindole-2- 2H), 2.18 (t, J = 7.1 Hz, 2H) carboxamide 842 N-[4-(2,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.73- (ESI(+)) diazaspiro[3.5]non-7- 7.53 (m, 2H), 7.42-7.31 (m, 4H), 7.31- m/e 391 ylcarbonyl)phenyl]- 7.25 (m, 2H), 4.79 (s, 4H), 3.81 (d, J = 5.0 (M + H)⁺ 1,3-dihydro-2H- Hz, 4H), 3.44 (dd, J = 12.2, 6.6 Hz, 4H), isoindole-2- 1.92-1.53 (m, 4H) carboxamide 843 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.67- (ESI(+)) diazaspiro[3.5]non-2- 7.61 (m, 2H), 7.58-7.54 (m, 2H), 7.39- m/e 391 ylcarbonyl)phenyl]- 7.29 (m, 4H), 4.79 (s, 4H), 4.07 (d, J = 7.8 (M + H)⁺ 1,3-dihydro-2H- Hz, 2H), 3.95 (d, J = 22.6 Hz, 2H), 2.99 (t, J = isoindole-2- 11.8, 6.0 Hz, 2H), 2.55 (s, 2H), 1.97-1.82 carboxamide (m, 2H), 1.82-1.59 (m, 2H) 844 N-[4-(1,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.72- (ESI(+)) diazaspiro[4.4]non-1- 7.57 (m, 2H), 7.50-7.40 (m, 2H), 7.40- m/e 391 ylcarbonyl)phenyl]- 7.22 (m, 4H), 4.79 (s, 4H), 3.83 (d, J = 12.2 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 3.75-3.63 (m, 1H), 3.57-3.42 isoindole-2- (m, 2H), 3.17 (t, J = 13.0 Hz, 1H), 2.61 (m, J = carboxamide 13.5, 9.0 Hz, 1H), 2.27-1.99 (m, 3H), 1.92-1.61 (m, 2H) 845 N-[4-(1,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.77- (ESI(+)) diazaspiro[4.4]non-7- 7.56 (m, 2H), 7.54-7.42 (m, 2H), 7.41- m/e 391 ylcarbonyl)phenyl]- 7.22 (m, 4H), 4.79 (s, 4H), 3.88 (d, J = 12.7 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 3.75-3.56 (m, 3H), 2.39-2.25 isoindole-2- (m, 1H), 2.26-2.11 (m, 1H), 2.10-1.87 (m, carboxamide 4H) 846 N-[4-(2,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.70- (ESI(+)) diazaspiro[4.4]non-2- 7.54 (m, 2H), 7.50-7.40 (m, 2H), 7.39- m/e 391 ylcarbonyl)phenyl]- 7.22 (m, 4H), 4.79 (s, 4H), 3.72-3.42 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.17 (t, J = 10.1 Hz, 2H), 2.14-1.81 isoindole-2- (m, 4H) carboxamide 847 N-[4-(2,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.70- (ESI(+)) diazaspiro[4.5]dec-2- 7.55 (m, 2H), 7.52-7.40 (m, 2H), 7.38- m/e 405 ylcarbonyl)phenyl]- 7.16 (m, 4H), 4.79 (s, 4H), 3.57 (t, J = 7.2 (M + H)⁺ 1,3-dihydro-2H- Hz, 2H), 3.41 (s, 2H), 3.15-2.98 (m, 4H), isoindole-2- 2.53-2.50 (m, 2H), 1.82 (t, 2H), 1.76-1.60 carboxamide (m, 4H) 848 N-[4-(2,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.71- (ESI(+)) diazaspiro[4.5]dec-2- 7.54 (m, 2H), 7.53-7.39 (m, 2H), 7.39- m/e 405 ylcarbonyl)phenyl]- 7.20 (m, 4H), 4.79 (s, 4H), 3.63-3.55 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 3.55-3.47 (m, 1H), 3.46-3.39 (m, isoindole-2- 1H), 3.07-2.98 (m, 4H), 1.98-1.87 (m, carboxamide 1H), 1.86-1.77 (m, 1H), 1.77-1.71 (m, 1H), 1.71-1.56 (m, 3H) 849 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.76- (ESI(+)) diazaspiro[4.5]dec-2- 7.55 (m, 2H), 7.55-7.41 (m, 2H), 7.41- m/e 405 ylcarbonyl)phenyl]- 7.20 (m, 4H), 4.79 (s, 4H), 3.82 (d, J = 12.8 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 3.77-3.66 (m, 1H), 3.66-3.53 isoindole-2- (m, 2H), 3.17-2.98 (m, 2H), 2.36-2.21 (m, carboxamide 1H), 2.19-2.06 (m, 1H), 1.87-1.77 (m, 2H), 1.76-1.55 (m, 4H) 850 N-[4-(2,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.76- (ESI(+)) diazaspiro[4.5]dec-7- 7.55 (m, 2H), 7.45-7.32 (m, 3H), 7.34- m/e 405 ylcarbonyl)phenyl]- 7.19 (m, 4H), 4.79 (s, 4H), 3.66-3.49 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 3.47-3.36 (m, 1H), 3.27-3.12 (m, isoindole-2- 1H), 3.10-2.90 (m, 2H), 2.00-1.83 (m, carboxamide 1H), 1.84-1.62 (m, 3H), 1.62-1.46 (m, 2H) 851 N-[4-(3,9- (ESI(+)) diazaspiro[5.5]undec-3- m/e XXX ylcarbonyl)phenyl]- (M + H)⁺ 1,3-dihydro-2H- isoindole-2- carboxamide 852 N-[4-(2,9- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.78- (ESI(+)) diazaspiro[5.5]undec-2- 7.54 (m, 2H), 7.46-7.21 (m, 6H), 4.79 (s, m/e 419 ylcarbonyl)phenyl]- 4H), 3.66 (d, J = 13.3 Hz, 1H), 3.54 (d, J = (M + H)⁺ 1,3-dihydro-2H- 14.2 Hz, 1H), 3.35 (dd, J = 14.9, 8.0 Hz, isoindole-2- 2H), 3.09-3.00 (m, 1H), 3.00-2.94 (m, carboxamide 1H), 2.94-2.85 (m, 2H), 2.54-2.48 (m, 2H), 1.70 (dd, J = 11.6, 5.7 Hz, 2H), 1.63 (dd, J = 16.4, 6.3 Hz, 2H), 1.61-1.50 (m, 4H), 1.50-1.39 (m, 1H) 853 N-[4-(2,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.79- (ESI(+)) diazaspiro[5.5]undec-2- 7.49 (m, 2H), 7.44-7.13 (m, 6H), 4.79 (s, m/e 419 ylcarbonyl)phenyl]- 4H), 3.45 (d, J = 9.0 Hz, 4H), 3.17-2.85 (M + H)⁺ 1,3-dihydro-2H- (m, 4H), 1.59 (dd, J = 12.8, 6.9 Hz, 8H) isoindole-2- carboxamide 854 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.74- (ESI(+)) diazaspiro[5.5]undec-8- 7.52 (m, 2H), 7.41-7.24 (m, 6H), 4.79 (s, m/e 419 ylcarbonyl)phenyl]- 4H), 3.82 (t, J = 14.5 Hz, 1H), 3.70 (d, J = (M + H)⁺ 1,3-dihydro-2H- 13.7 Hz, 1H), 3.55-3.40 (m, 2H), 3.16- isoindole-2- 2.88 (m, 2H), 2.01-1.81 (m, 2H), 1.75- carboxamide 1.53 (m, 8H) 855 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.73- (ESI(+)) diazaspiro[4.6]undec-8- 7.51 (m, 2H), 7.45-7.15 (m, 6H), 4.79 (s, m/e 419 ylcarbonyl)phenyl]- 4H), 3.77-3.59 (m, 1H), 3.62-3.36 (m, (M + H)⁺ 1,3-dihydro-2H- 3H), 3.29-3.20 (m, 2H), 2.12-1.95 (m, isoindole-2- 4H), 1.91-1.66 (m, 5H) carboxamide 856 N-{4-[(1-oxa-8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.78- (ESI(+)) azaspiro[4.5]dec-2- 7.72 (m, 2H), 7.66-7.61 (m, 2H), 7.39- m/e 435 ylmethyl)carbamoyl] 7.28 (m, 4H), 4.79 (s, 4H), 4.15 (dd, J = (M + H)⁺ phenyl}-1,3-dihydro- 12.2, 6.0 Hz, 1H), 3.38 (qd, J = 13.4, 5.8 Hz, 2H-isoindole-2- 2H), 3.20-3.00 (m, 4H), 2.53-2.50 (m, carboxamide 3H), 2.18-1.96 (m, 1H), 1.94-1.56 (m, 8H) 857 N-[4-(1-oxa-8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.84- (ESI(+)) azaspiro[4.5]dec-3- 7.70 (m, 2H), 7.70-7.54 (m, 2H), 7.46- m/e 421 ylcarbamoyl)phenyl]- 7.21 (m, 4H), 4.79 (s, 4H), 4.64-4.44 (m, (M + H)⁺ 1,3-dihydro-2H- 1H), 4.15-3.95 (m, 1H), 3.73 (dd, J = 9.1, isoindole-2- 6.1 Hz, 1H), 3.19-2.97 (m, 4H), 2.21 (dd, J = carboxamide 13.1, 8.3 Hz, 1H), 1.99-1.84 (m, 3H), 1.84-1.70 (m, 2H) 858 N-{4-[(2-oxa-9- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.87- (ESI(+)) azaspiro[5.5]undec-3- 7.69 (m, 2H), 7.71-7.53 (m, 2H), 7.45- m/e 449 ylmethyl)carbamoyl] 7.12 (m, 4H), 4.79 (s, 4H), 3.75 (dd, J = (M + H)⁺ phenyl}-1,3-dihydro- 11.5, 2.6 Hz, 1H), 3.55-3.41 (m, 1H), 3.38- 2H-isoindole-2- 3.31 (m, 2H), 3.22-3.12 (m, 1H), 3.11- carboxamide 2.94 (m, 4H), 1.92-1.66 (m, 3H), 1.62- 1.49 (m, 1H), 1.49-1.24 (m, 4H) 859 N-[4-(1-oxa-4,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.75- (ESI(+)) diazaspiro[5.5]undec-4- 7.53 (m, 2H), 7.44-7.15 (m, 6H), 4.79 (s, m/e 421 ylcarbonyl)phenyl]- 4H), 3.82-3.66 (m, 2H), 3.63-3.46 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.40-3.32 (m, 1H), 3.25-3.14 (m, isoindole-2- 1H), 2.96-2.77 (m, 2H), 2.08-1.92 (m, carboxamide 1H), 1.92-1.74 (m, 1H), 1.73-1.58 (m, 1H), 1.59-1.38 (m, 1H) 860 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.71- (ESI(+)) diazaspiro[4.5]dec-1- 7.48 (m, 2H), 7.45-7.18 (m, 6H), 4.79 (s, m/e 405 ylcarbonyl)phenyl]- 4H), 3.44 (t, J = 6.7 Hz, 2H), 3.36 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 7.3, 5.1 Hz, 1H), 3.24-3.06 (m, 2H), 3.05- isoindole-2- 2.85 (m, 2H), 2.05 (t, J = 7.0 Hz, 2H), 1.88- carboxamide 1.72 (m, 2H), 1.65 (dd, J = 12.7, 1.4 Hz, 2H) 861 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.75- (ESI(+)) diazaspiro[4.5]dec-8- 7.51 (m, 2H), 7.42-7.10 (m, 6H), 4.79 (s, m/e 405 ylcarbonyl)phenyl]- 4H), 3.92-3.68 (m, 2H), 3.36 (dd, J = 8.1, (M + H)⁺ 1,3-dihydro-2H- 5.4 Hz, 1H), 3.31-3.21 (m, 2H), 2.14-1.91 isoindole-2- (m, 4H), 1.91-1.68 (m, 4H) carboxamide 862 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.72- (ESI(+)) diazaspiro[3.4]oct-2- 7.60 (m, 2H), 7.60-7.49 (m, 2H), 7.42- m/e 377 ylcarbonyl)phenyl]- 7.21 (m, 4H), 4.79 (s, 4H), 4.20 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 29.4, 9.1 Hz, 4H), 3.42 (s, 2H), 3.27 (d, J = isoindole-2- 3.7 Hz, 1H), 3.24 (s, 1H), 2.24 (t, J = 7.4 Hz, carboxamide 2H) 863 N-[4-(1,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.72- (ESI(+)) diazaspiro[3.5]non-7- 7.52 (m, 2H), 7.43-7.10 (m, 6H), 5.54 (s, m/e 390 ylcarbonyl)phenyl]- 1H), 4.79 (s, 4H), 3.99 (d, J = 1 1.5 Hz, 2H), (M + H)⁺ 1,3-dihydro-2H- 3.68-3.49 (m, 2H), 2.95 (t, J = 7.4 Hz, 2H), isoindole-2- 2.53-2.51 (m, 1H), 2.41-2.25 (m, 2H), carboxamide 2.07 (t, J = 31.9 Hz, 2H) 864 N-[4-(1,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.75- (ESI(+)) diazaspiro[3.5]non-1- 7.61 (m, 2H), 7.60-7.48 (m, 2H), 7.42- m/e 391 ylcarbonyl)phenyl]- 7.12 (m, 4H), 4.79 (s, 4H), 4.54-4.29 (m, (M + H)⁺ 1,3-dihydro-2H- 1H), 4.14-3.91 (m, 1H), 3.86-3.55 (m, isoindole-2- 1H), 3.26-3.18 (m, 1H), 3.12-2.79 (m, carboxamide 1H), 2.50 (dd, J = 9.4, 1.3 Hz, 1H), 2.43- 2.20 (m, 1H), 2.17-2.01 (m, 1H), 2.01- 1.85 (m, 2H), 1.87-1.52 (m, 1H) 865 N-[4-(2,5- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.75- (ESI(+)) diazaspiro[3.5]non-2- 7.62 (m, 2H), 7.62-7.52 (m, 2H), 7.44- m/e 391 ylcarbonyl)phenyl]- 7.18 (m, 4H), 4.80 (s, 4H), 4.28 (d, J = 10.2 (M + H)⁺ 1,3-dihydro-2H- Hz, 2H), 4.19 (s, 2H), 3.10 (t, J = 5.3 Hz, isoindole-2- 2H), 2.01 (t, J = 5.4 Hz, 2H), 1.77-1.35 (m, carboxamide 4H) 866 N-[4-(5-oxa-2- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) azaspiro[3.4]oct-2- 7.60 (m, 2H), 7.57-7.53 (m, 2H), 7.40- m/e 378 ylcarbonyl)phenyl]- 6.97 (m, 5H), 4.79 (s, 5H), 4.16 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 23.4, 9.6 Hz, 4H), 3.77 (t, J = 6.8 Hz, 2H), isoindole-2- 3.35 (q, J = 7.1 Hz, 1H), 2.07 (dd, J = 8.1, carboxamide 6.6 Hz, 2H), 1.98-1.74 (m, 2H), 1.11 (t, J = 7.1 Hz, 1H) 867 N-[4-(6-oxa-2- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) azaspiro[3.5]non-2- 7.60 (m, 2H), 7.58-7.54 (m, 2H), 7.38- m/e 392 ylcarbonyl)phenyl]- 7.28 (m, 4H), 4.79 (s, 4H), 3.95-3.67 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.59 (s, 2H), 3.55-3.44 (m, 2H), 1.90- isoindole-2- 1.72 (m, 2H), 1.61-1.39 (m, 2H) carboxamide 868 N-[4-(hexahydro-5H- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.75- (ESI(+)) furo[2,3-c]pyrrol-5- 7.52 (m, 2H), 7.46-7.20 (m, 6H), 4.79 (s, m/e 378 ylcarbonyl)phenyl]- 4H), 4.49-4.27 (m, 1H), 3.95-3.78 (m, (M + H)⁺ 1,3-dihydro-2H- 1H), 3.77-3.55 (m, 4H), 3.43 (dd, J = 11.8, isoindole-2- 5.4 Hz, 1H), 2.98-2.70 (m, 1H), 2.06 (ddd, carboxamide J = 15.0, 12.5, 7.7 Hz, 1H), 1.82-1.49 (m, 1H) 869 N-[4-(tetrahydro-1H- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.69- (ESI(+)) furo[3,4-c]pyrrol- 7.61 (m, 1H), 7.60 (d, 1H), 7.47-7.07 (m, m/e 378 5(3H)- 6H), 4.79 (s, 4H) , 3.83-3.59 (m, 4H), 3.58- (M + H)⁺ ylcarbonyl)phenyl]- 3.33 (m, 4H), 3.05-2.82 (m, 2H) 1,3-dihydro-2H- isoindole-2- carboxamide 870 N-[4- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.71- (ESI(+)) (hexahydrofuro[3,4- 7.52 (m, 2H), 7.41-7.12 (m, 6H), 4.79 (s, m/e 392 c]pyridin-5(3H)- 4H), 3.89-3.65 (m, 2H), 3.67-3.40 (m, (M + H)⁺ ylcarbonyl)phenyl]- 5H), 3.39-3.26 (m, 1H), 2.46-2.25 (m, 1,3-dihydro-2H- 2H), 1.88-1.63 (m, 1H), 1.67-1.24 (m, 1H) isoindole-2- carboxamide 885 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.68- (ESI(+)) diazaspiro[3.4]oct-6- 7.51 (m, 2H), 7.51-7.28 (m, 3H), 7.24- m/e 393 ylcarbonyl)phenyl]- 7.00 (m, 1H), 4.77 (d, J = 12.1 Hz, 4H), 3.61 (M + H)⁺ 5-fluoro-1,3-dihydro- (d, J = 17.1 Hz, 2H), 3.54 (d, J = 8.2 Hz, 2H-isoindole-2- 3H), 3.48 (t, J = 7.0 Hz, 2H), 2.06 (dd, J = carboxamide 23.6, 16.6 Hz, 2H), 1.89 (s, 1H) 886 N-[4-(2,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) diazaspiro[3.5]non-7- 7.53 (m, 2H), 7.37 (dd, J = 8.3, 5.2 Hz, 1H), m/e 407 ylcarbonyl)phenyl]- 7.31-7.22 (m, 2H), 7.17 (d, J = 9.0 Hz, (M + H)⁺ 5-fluoro-1,3-dihydro- 1H), 7.15-6.92 (m, 1H), 4.77 (d, J = 12.3 2H-isoindole-2- Hz, 4H), 3.41 (t, J = 5.5 Hz, 8H), 1.78-1.63 carboxamide (m, 4H) 887 N-[4-(1,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) diazaspiro[4.4]non-1- 7.49 (m, 2H), 7.43-7.32 (m, 3H), 7.22- m/e 409 ylcarbonyl)phenyl]- 7.03 (m, 2H), 4.76 (d, J = 12.6 Hz, 4H), 3.54- (M + H)⁺ 5-fluoro-1,3-dihydro- 3.37 (m, 2H), 2.86 (dt, J = 11.3, 7.9 Hz, 2H-isoindole-2- 1H), 2.70 (d, J = 11.7 Hz, 1H), 2.10-1.96 carboxamide (m, 1H), 1.90 (d, J = 29.4 Hz, 1H), 1.84- 1.67 (m, 2H), 1.25 (s, 1H) 888 N-[4-(2,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.70- (ESI(+)) diazaspiro[4.5]dec-2- 7.49 (m, 2H), 7.45-7.32 (m, 3H), 7.22- m/e 423 ylcarbonyl)phenyl]- 7.03 (m, 2H), 4.77 (d, J = 12.4 Hz, 4H), 3.53 (M + H)⁺ 5-fluoro-1,3-dihydro- (t, J = 7.2 Hz, 2H), 3.33 (s, 2H), 2.79 (dd, J = 2H-isoindole-2- 20.6, 14.7 Hz, 3H), 1.88 (s, 1H), 1.78 (t, J = carboxamide 7.1 Hz, 2H), 1.50 (s, 4H) 889 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.70- (ESI(+)) diazaspiro[4.5]dec-2- 7.54 (m, 2H), 7.50-7.30 (m, 3H), 7.24- m/e 423 ylcarbonyl)phenyl]- 7.00 (m, 2H), 4.77 (d, J = 12.5 Hz, 4H), 3.75- (M + H)⁺ 5-fluoro-1,3-dihydro- 3.54 (m, 1H), 3.57-3.47 (m, 2H), 3.40 (d, 2H-isoindole-2- J = 11.8 Hz, 1H), 3.20 (d, J = 0.5 Hz, 1H), carboxamide 2.76 (d, J = 21.5 Hz, 2H), 2.07-1.77 (m, 3H), 1.64-1.40 (m, 6H) 890 N-[4-(2,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.69- (ESI(+)) diazaspiro[4.5]dec-7- 7.54 (m, 2H), 7.37 (dd, J = 8.4, 5.2 Hz, 1H), m/e 423 ylcarbonyl)phenyl]- 7.33-7.22 (m, 2H), 7.23-7.02 (m, 2H), (M + H)⁺ 5-fluoro-1,3-dihydro- 4.77 (d, J = 12.2 Hz, 4H), 3.53-3.31 (m, 2H-isoindole-2- 4H), 3.20 (s, 2H), 2.94-2.79 (m, 2H), 2.64 carboxamide (dd, J = 42.4, 11.2 Hz, 2H), 1.87 (s, 2H), 1.74-1.32 (m, 6H) 891 N-[4-(2,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.59 (ESI(+)) diazaspiro[5.5]undec-2- (dd, J = 6.4, 4.5 Hz, 2H), 7.37 (dd, J = 8.4, m/e 437 ylcarbonyl)phenyl]- 5.1 Hz, 1H), 7.33-7.20 (m, 2H), 7.17 (d, J = (M + H)⁺ 5-fluoro-1,3-dihydro- 9.0 Hz, 1H), 7.13-7.02 (m, 1H), 4.77 (d, 2H-isoindole-2- J = 12.4 Hz, 4H), 3.51-3.36 (m, 4H), 3.20 carboxamide (s, 2H), 2.80-2.65 (m, 2H), 2.64 (s, 2H), 1.85 (s, 2H), 1.52 (s, 4H), 1.37 (t, J = 5.7 Hz, 4H) 892 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) diazaspiro[5.5]undec-8- 7.51 (m, 2H), 7.37 (dd, J = 8.4, 5.1 Hz, 1H), m/e 437 ylcarbonyl)phenyl]- 7.34-7.24 (m, 2H), 7.23-7.05 (m, 2H), (M + H)⁺ 5-fluoro-1,3-dihydro- 4.77 (d, J = 12.5 Hz, 4H), 3.58-3.36 (m, 2H-isoindole-2- 4H), 3.20 (s, 2H), 2.72-2.54 (m, 2H), 1.62- carboxamide 1.36 (m, 8H) 893 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) diazaspiro[4.6]undec-8- 7.51 (m, 2H), 7.37 (dd, J = 8.3, 5.2 Hz, 1H), m/e 437 ylcarbonyl)phenyl]- 7.32-7.23 (m, 2H), 7.19-7.01 (m, 2H), (M + H)⁺ 5-fluoro-1,3-dihydro- 4.77 (d, J = 12.9 Hz, 4H), 3.49 (d, J = 14.0 2H-isoindole-2- Hz, 3H), 3.03-2.76 (m, 2H), 1.84-1.59 carboxamide (m, 8H), 1.25 (s, 6H) 894 5-fluoro-N-{4-[(1- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.83- (ESI(+)) oxa-8- 7.68 (m, 2H), 7.68-7.49 (m, 2H), 7.37 (dd, m/e 453 azaspiro[4.5]dec-2- J = 8.4, 5.1 Hz, 1H), 7.21-6.93 (m, 2H), (M + H)⁺ ylmethyl)carbamoyl] 4.77 (d, J = 12.2 Hz, 4H), 4.10 (t, J = 6.0 Hz, phenyl}-1,3-dihydro- 1H), 3.44-3.31 (m, 2H), 3.06-2.83 (m, 2H-isoindole-2- 2H), 2.83-2.70 (m, 2H), 2.12-1.92 (m, carboxamide 1H), 1.81-1.66 (m, 3H), 1.62-1.32 (m, 4H) 895 5-fluoro-N-[4-(1- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.80- (ESI(+)) oxa-8- 7.69 (m, 2H), 7.66-7.50 (m, 2H), 7.37 (dd, m/e 439 azaspiro[4.5]dec-3- J = 8.2, 5.1 Hz, 1H), 7.27-6.90 (m, 2H), (M + H)⁺ ylcarbamoyl)phenyl]- 4.77 (d, J = 12.7 Hz, 4H), 4.61-4.39 (m, 1,3-dihydro-2H- 1H), 4.02 (dd, J = 8.9, 6.8 Hz, 1H), 3.66 (dd, isoindole-2- J = 8.9, 6.3 Hz, 1H), 3.01-2.81 (m, 2H), carboxamide 2.80-2.61 (m, 2H), 2.15 (dd, J = 12.9, 8.3 Hz, 1H), 1.87-1.73 (m, 1H), 1.70 (t, J = 5.7 Hz, 2H), 1.65-1.49 (m, 2H) 896 5-fluoro-N-[4-(1- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.69- (ESI(+)) oxa-4,8- 7.54 (m, 2H), 7.37 (dd, J = 8.3, 5.1 Hz, 1H), m/e 439 diazaspiro[5.5]undec-4- 7.35-7.28 (m, 2H), 7.17 (d, J = 9.0 Hz, (M + H)⁺ ylcarbonyl)phenyl]- 1H), 7.14-6.96 (m, 1H), 4.77 (d, J = 12.4 1,3-dihydro-2H- Hz, 4H), 3.77-3.57 (m, 2H), 3.57-3.36 isoindole-2- (m, 4H), 2.71 (dd, J = 25.6, 8.7 Hz, 1H), carboxamide 2.62 (d, J = 13.1 Hz, 3H), 1.90(s, 1H), 1.81- 1.43 (m, 3H), 1.31 (s, 1H) 897 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.61- (ESI(+)) diazaspiro[4.5]dec-1- 7.51 (m, 2H), 7.37 (dd, J = 8.3, 5.2 Hz, 1H), m/e 423 ylcarbonyl)phenyl]- 7.33-7.25 (m, 2H), 7.16 (d, J = 9.0 Hz, (M + H)⁺ 5-fluoro-1,3-dihydro- 1H), 7.10 (dd, J = 12.4, 5.4 Hz, 1H), 4.76 (d, 2H-isoindole-2- J = 13.0 Hz, 4H), 3.39 (t, J = 6.7 Hz, 2H), carboxamide 3.06 (d, J = 12.4 Hz, 2H), 3.00-2.82 (m, 2H), 2.79-2.61 (m, 2H), 1.99 (t, J = 6.9 Hz, 2H), 1.88 (s, 1H), 1.73 (dd, J = 13.6, 6.9 Hz, 2H), 1.44 (d, J = 13.3 Hz, 2H) 898 N-[4-(1,8- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.71- (ESI(+)) diazaspiro[4.5]dec-8- 7.51 (m, 2H), 7.37 (dd, J = 8.4, 5.2 Hz, 1H), m/e 423 ylcarbonyl)phenyl]- 7.33-7.23 (m, 2H), 7.22-7.12 (m, 1H), (M + H)⁺ 5-fluoro-1,3-dihydro- 7.09 (dd, J = 13.2, 4.7 Hz, 1H), 4.77 (d, J = 2H-isoindole-2- 12.6 Hz, 4H), 3.62-3.39 (m, 4H), 3.00- carboxamide 2.75 (m, 2H), 1.86-1.67 (m, 2H), 1.67- 1.43 (m, 6H) 899 N-[4-(2,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.68- (ESI(+)) diazaspiro[3.4]oct-2- 7.49 (m, 4H), 7.37 (dd, J = 8.5, 5.2 Hz, 1H), m/e 395 ylcarbonyl)phenyl]- 7.23-7.04 (m, 2H), 4.77 (d, J = 12.3 Hz, (M + H)⁺ 5-fluoro-1,3-dihydro- 4H), 4.10 (s, 4H), 3.00 (s, 2H), 2.83 (dd, J = 2H-isoindole-2- 46.1, 39.1 Hz, 2H), 1.98 (t, J = 7.1 Hz, 2H) carboxamide 900 N-[4-(1,7- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.70- (ESI(+)) diazaspiro[3.5]non-7- 7.53 (m, 2H), 7.48-7.23 (m, 3H), 7.23- m/e 409 ylcarbonyl)phenyl]- 7.03 (m, 2H), 5.45 (s, 1H), 4.77 (d, J = 12.2 (M + H)⁺ 5-fluoro-1,3-dihydro- Hz, 4H), 3.98 (s, 2H), 3.56 (t, J = 5.7 Hz, 2H-isoindole-2- 2H), 2.71 (t, J = 7.1 Hz, 2H), 2.32-2.05 (m, carboxamide 4H), 1.86 (s, 2H) 901 N-[4-(1,6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.69- (ESI(+)) diazaspiro[3.5]non-1- 7.52 (m, 2H), 7.47 (d, J = 8.6 Hz, 2H), 7.37 m/e 409 ylcarbonyl)phenyl]- (dd, J = 8.4, 5.1 Hz, 1H), 7.22-7.01 (m, (M + H)⁺ 5-fluoro-1,3-dihydro- 2H), 4.77 (d, J = 12.9 Hz, 4H), 4.24-3.92 2H-isoindole-2- (m, 2H), 3.20 (s, 3H), 2.97 (t, J = 18.2 Hz, carboxamide 1H), 2.75 (t, J = 21.1 Hz, 1H), 2.29-2.11 (m, 1H), 2.10-1.96 (m, 1H), 1.62 (s, 1H), 1.49 (d, J = 11.0 Hz, 1H) 902 N-[4-(2,5- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.69- (ESI(+)) diazaspiro[3.5]non-2- 7.50 (m, 4H), 7.37 (dd, J = 8.6, 5.2 Hz, 1H), m/e 409 ylcarbonyl)phenyl]- 7.22-7.03 (m, 2H), 4.77 (d, J = 13.2 Hz, (M + H)⁺ 5-fluoro-1,3-dihydro- 4H), 3.92 (s, 4H), 2.66 (dd, J = 10.8, 5.5 Hz, 2H-isoindole-2- 2H), 1.70-1.59 (m, 2H), 1.51 (s, 2H), 1.40 carboxamide (d, J = 4.6 Hz, 2H) 903 5-fluoro-N-[4-(5- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.71- (ESI(+)) oxa-2- 7.47 (m, 4H), 7.37 (dd, J = 8.4, 5.2 Hz, 1H), m/e 396 azaspiro[3.4]oct-2- 7.22-6.96 (m, 2H), 4.77 (d, J = 12.5 Hz, (M + H)⁺ ylcarbonyl)phenyl]- 4H), 4.16 (dd, J = 23.5, 9.7 Hz, 4H), 3.77 (t, 1,3-dihydro-2H- J = 6.8 Hz, 2H), 2.07 (t, J = 7.3 Hz, 2H), isoindole-2- 1.94-1.70 (m, 2H) carboxamide 904 5-fluoro-N-[4-(6- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.68- (ESI(+)) oxa-2- 7.51 (m, 2H), 7.5 1-7.33 (m, 1H), 7.36- m/e 410 azaspiro[3.5]non-2- 7.20 (m, 2H), 7.21-6.92 (m, 2H), 4.77 (d, J = (M + H)⁺ ylcarbonyl)phenyl]- 12.5 Hz, 4H), 4.24 (dd, J = 26.5, 6.0 Hz, 1,3-dihydro-2H- 4H), 3.48-3.36 (m, 2H), 1.97-1.75 (m, isoindole-2- 2H), 1.66-1.25 (m, 4H) carboxamide 905 5-fluoro-N-[4-(2- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) oxa-7- 7.54 (m, 2H), 7.37 (dd, J = 8.3, 5.2 Hz, 1H), m/e 410 azaspiro[3.5]non-7- 7.35-7.23 (m, 2H), 7.22-7.03 (m, 2H), (M + H)⁺ ylcarbonyl)phenyl]- 4.77 (d, J = 12.4 Hz, 4H), 4.35 (s, 4H), 3.47- 1,3-dihydro-2H- 3.36 (m, 4H), 1.87-1.75 (m, 4H) isoindole-2- carboxamide 906 5-fluoro-N-[4- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.67- (ESI(+)) (hexahydro-5H- 7.54 (m, 2H), 7.48-7.28 (m, 3H), 7.24- m/e 396 furo[2,3-c]pyrrol-5- 6.92 (m, 2H), 4.77 (d, J = 12.4 Hz, 4H), 4.52- (M + H)⁺ ylcarbonyl)phenyl]- 4.31 (m, 1H), 3.86 (dd, J = 15.5, 7.0 Hz, 1,3-dihydro-2H- 1H), 3.79-3.53 (m, 4H), 3.43 (dd, J = 11.7, isoindole-2- 5.3 Hz, 1H), 2.97-2.81 (m, 1H), 2.17-1.88 carboxamide (m, 1H), 1.88-1.59 (m, 1H) 907 5-fluoro-N-[4- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.65- (ESI(+)) (tetrahydro-1H- 7.54 (m, 2H), 7.54-7.31 (m, 3H), 7.26- m/e 396 furo[3,4-c]pyrrol- 7.03 (m, 2H), 4.77 (d, J = 12.2 Hz, 4H), 3.74 (M + H)⁺ 5(3H)- (ddd, J = 19.7, 10.5, 7.2 Hz, 4H), 3.56-3.34 ylcarbonyl)phenyl]- (m, 4H), 3.01-2.84 (m, 2H) 1,3-dihydro-2H- isoindole-2- carboxamide 908 5-fluoro-N-[4- ¹H NMR (400 MHz, DMSO-D₂O) δ 7.59 (d, (ESI(+)) (hexahydrofuro[3,4- J = 8.7 Hz, 2H), 7.43-7.35 (m, 1H), 7.35- m/e 410 c]pyridin-5(3H)- 7.24 (m, 2H), 7.22-7.05 (m, 2H), 4.77 (d, J = (M + H)⁺ ylcarbonyl)phenyl]- 12.5 Hz, 4H), 3.81-3.67 (m, 2H), 3.62- 1,3-dihydro-2H- 3.40 (m, 4H), 1.76 (s, 1H), 1.62-1.36 (m, isoindole-2- 1H), 1.28-1.08 (m, 2H) carboxamide 976 N-(4-{[(1S)-1-(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.59 (s, (ESI(+)) fluorophenyl)-2- 1H), 8.49 (d, J = 8.0 Hz, 1H), 7.87-7.79 m/e 420 hydroxyethyl]carbamoyl}phenyl)- (m, 2H), 7.72-7.65 (m, 2H), 7.47-7.28 (m, (M + H)⁺ 1,3-dihydro-2H- 6H), 7.19-7.09 (m, 2H), 5.06 (d, J = 6.7 isoindole-2- Hz, 1H), 4.95-4.87 (m, 1H), 4.79 (s, 4H), carboxamide 3.77-3.57 (m, 2H) 977 N-(4-{[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.58 (d, J = (ESI(+)) hydroxy-1-(4- 3.8 Hz, 1H), 8.42 (d, J = 8.1 Hz, 1H), 7.86- m/e 432 methoxyphenyl)eth- 7.76 (m, 3H), 7.69 (s, 1H), 7.69-7.61 (m, (M + H)⁺ yl]carbamoyl}phenyl)- 2H), 7.41-7.27 (m, 6H), 6.91-6.84 (m, 1,3-dihydro-2H- 2H), 5.07-4.96 (m, 1H), 3.77-3.59 (m, isoindole-2- 4H), 3.31 (s, 4H) carboxamide 978 N-(4-{[(1S)-1-(1,3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.59 (s, (ESI(+)) benzodioxol-5-yl)-2- 1H), 8.39 (d, J = 8.1 Hz, 1H), 7.86-7.78 m/e 446 hydroxyethyl]carbamoyl}phenyl)- (m, 2H), 7.72-7.64 (m, 2H), 7.41-7.28 (m, (M + H)⁺ 1,3-dihydro-2H- 4H), 6.99 (s, 1H), 6.87-6.82 (m, 2H), 5.97 isoindole-2- (d, J = 2.3 Hz, 2H), 5.05-4.93 (m, 1H), carboxamide 4.92-4.82 (m, 1H), 4.81 (d, J = 14.1 Hz, 4H), 3.73-3.53 (m, 2H) 1089 5-fluoro-N-(4-{[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (1,3-thiazol-2- δ 7.78-7.64 (m, 2H), 7.64-7.53 (m, 2H), m/e 425 yl)propan-2- 7.52-7.34 (m, 1H), 7.28-7.16 (m, 1H), (M + H)⁺ yl]carbamoyl}phenyl)- 7.17-7.03 (m, 1H), 4.77 (d, J = 12.4 Hz, 1,3-dihydro-2H- 4H), 4.38 (h, J = 6.6 Hz, 1H), 3.41-3.27 isoindole-2- (m, 2H), 3.24-3.15 (m, 1H), 2.51 (dt, J = carboxamide 3.7, 1.9 Hz, 2H), 1.25 (t, J = 5.6 Hz, 3H), 1.11 (t, J = 7.1 Hz, 1H) 1090 N-{4-[(4,4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) difluorocyclohexyl)carbamoyl]phe- δ 7.86-7.70 (m, 2H), 7.67-7.53 (m, 2H), m/e 418 nyl}-5-fluoro-1,3-dihydro- 7.44-7.29 (m, 1H), 7.24-7.03 (m, 2H), (M + H)⁺ 2H-isoindole-2- 4.76 (t, J = 10.2 Hz, 4H), 4.08-3.87 (m, carboxamide 1H), 2.16-1.83 (m, 5H), 1.79-1.54 (m, 2H) 1091 N-(4-{[1-(3,5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethyl-1H- δ 7.81-7.65 (m, 2H), 7.65-7.55 (m, 2H), m/e 436 pyrazol-1-yl)propan-2- 7.41-7.31 (m, 1H), 7.23-6.98 (m, 2H), (M + H)⁺ yl]carbamoyl}phenyl)- 4.77 (d, J = 12.4 Hz, 4H), 4.35 (h, J = 6.5 5-fluoro-1,3- Hz, 1H), 4.17-4.06 (m, 1H), 4.06-3.88 dihydro-2H- (m, 1H), 3.20 (s, 1H), 2.22 (s, 3H), 2.10 (s, isoindole-2- 3H), 1.26-1.01 (m, 3H) carboxamide 1092 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-2- δ 7.87-7.71 (m, 2H), 7.69-7.58 (m, 2H), m/e 455 (morpholin-4- 7.46-7.29 (m, 1H), 7.25-7.02 (m, 2H), (M + H)⁺ yl)butyl]carbamoyl} 4.89-4.69 (m, 4H), 3.90-3.67 (m, 4H), phenyl)-1,3-dihydro- 3.61-3.41 (m, 2H), 3.15-2.96 (m, 2H), 2H-isoindole-2- 1.84-1.50 (m, 2H), 1.32-1.06 (m, 3H), carboxamide 1.07-0.72 (m, 3H) 1093 5-fluoro-N-(4-{[2-(2- ¹H NMR (400 MHz, Pyridine-d₅) δ 8.59- (ESI(+)) methyl-1,3-thiazol-4- 8.46 (m, 2H), 7.90 (d, J = 8.6 Hz, 2H), 7.68- m/e 425 yl)ethyl]carbamoyl}phenyl)- 7.58 (m, 2H), 7.10 (d, J = 5.0 Hz, 1H), (M + H)⁺ 1,3-dihydro- 4.87 (dd, J = 16.8, 9.9 Hz, 4H), 3.86-3.64 2H-isoindole-2- (m, 4H), 3.64-3.40 (m, 5H), 2.86-2.58 (m, carboxamide 2H) 1094 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1- δ 7.70 (d, J = 8.7 Hz, 2H), 7.66-7.54 (m, m/e 425 (morpholin-4- 2H), 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.21- (M + H)⁺ yl)propan-2- 7.05 (m, 2H), 4.77 (d, J = 12.5 Hz, 4H), 3.65 yl]carbamoyl}phenyl)- (s, 4H), 2.80 (d, J = 54.6 Hz, 5H), 1.41 (s, 6H) 1,3-dihydro-2H- isoindole-2- carboxamide 1095 5-fluoro-N-{4-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- δ 7.89-7.70 (m, 2H), 7.70-7.52 (m, 2H), m/e 420 1,3-dihydro-2H- 7.37 (dd, J = 8.3, 5.2 Hz, 1H), 7.26 (d, J = (M + H)⁺ isoindole-2- 8.6 Hz, 2H), 7.20-7.04 (m, 2H), 6.93-6.76 carboxamide (m, 2H), 4.77 (d, J = 12.5 Hz, 4H), 4.41 (s, 2H), 3.74 (s, 3H) 1096 5-fluoro-N-(4-{[3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (morpholin-4- δ 7.83-7.70 (m, 2H), 7.69-7.55 (m, 2H), m/e 427 yl)propyl]carbamoyl}phenyl)- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.27-7.03 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 4.77 (d, J = 12.4 Hz, 4H), 3.86 (s, isoindole-2- 4H), 3.36 (dd, J = 17.9, 1 1.2 Hz, 3H), 3.22- carboxamide 3.09 (m, 3H), 2.09-1.81 (m, 2H) 1097 N-alpha-(4-{[(5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) fluoro-1,3-dihydro- δ 7.76-7.64 (m, 2H), 7.64-7.52 (m, 2H), m/e 447 2H-isoindol-2- 7.44-7.31 (m, 1H), 7.31-7.21 (m, 4H), (M + H)⁺ yl)carbonyl]amino}benzoyl)-D- 7.21-7.04 (m, 3H), 4.82-4.73 (m, 4H), phenylalaninamide 4.73-4.62 (m, 1H), 3.23-3.12 (m, 2H), 3.07-2.93 (m, 2H) 1098 N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (acetylamino)phenyl] δ 7.96-7.78 (m, 2H), 7.77-7.64 (m, 3H), m/e 433 carbamoyl}phenyl)- 7.51-7.42 (m, 1H), 7.42-7.31 (m, 1H), (M + H)⁺ 5-fluoro-1,3-dihydro- 7.28-7.15 (m, 3H), 7.15-7.03 (m, 1H), 2H-isoindole-2- 4.86-4.70 (m, 4H), 2.09 (s, 3H) carboxamide 1099 5-fluoro-N-[4-({4-[2-(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) hydroxyethoxy)ethyl]piperazin- δ 7.71-7.57 (m, 2H), 7.50-7.33 (m, 3H), m/e 457 1-yl}carbonyl)phenyl]- 7.25-7.01 (m, 2H), 4.77 (d, J = 12.5 Hz, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.65-3.47 (m, 4H), 3.35 (dd, J = 12.2, isoindole-2- 7.3 Hz, 6H), 2.52 (dt, J = 3.8, 1.9 Hz, 2H) carboxamide 1100 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (furan-2-yl)-2- δ 7.76-7.67 (m, 3H), 7.66-7.53 (m, 2H), m/e 463 (pyrrolidin-1- 7.37 (dd, J = 8.4, 5.2 Hz, 1H), 7.25-7.02 (M + H)⁺ yl)ethyl]carbamoyl}phenyl)- (m, 2H), 6.78 (d, J = 3.3 Hz, 1H), 6.55 (dd, J = 1,3-dihydro- 3.3, 1.9 Hz, 1H), 4.89-4.68 (m, 6H), 4.08- 2H-isoindole-2- 3.94 (m, 1H), 3.87 (dd, J = 14.0, 7.4 Hz, carboxamide 1H), 3.43 (s, 1H), 2.00-1.78 (m, 4H) 1101 N-{4-[bis(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxyethyl)carbamoyl]phenyl}- δ 7.58 (d, J = 8.6 Hz, 2H), 7.37 (dd, J = 8.3, m/e 416 5-fluoro-1,3-dihydro- 5.1 Hz, 1H), 7.31-7.22 (m, 2H), 7.17 (d, J = (M + H)⁺ 2H-isoindole-2- 8.9 Hz, 1H), 7.13-7.03 (m, 1H), 4.76 (d, carboxamide J = 12.5 Hz, 4H), 3.60-3.41 (m, 8H), 3.24 (s, 6H) 1102 N-{4-[(1-amino-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) oxohexan-2- δ 7.87-7.71 (m, 2H), 7.64 (t, J = 10.2 Hz, m/e 413 yl)carbamoyl]phenyl}- 2H), 7.46-7.31 (m, 1H), 7.23-7.03 (m, (M + H)⁺ 5-fluoro-1,3- 2H), 4.78 (d, J = 12.5 Hz, 4H), 4.40 (dd, J = dihydro-2H- 8.6, 5.6 Hz, 1H), 1.90-1.62 (m, 2H), 1.45- isoindole-2- 1.18 (m, 4H), 0.87 (t, J = 6.9 Hz, 3H) carboxamide 1103 N-(4-{[2-(3,4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethoxyphenyl)eth- δ 7.72 (d, J = 8.7 Hz, 2H), 7.60 (d, J = 8.7 m/e 464 yl]carbamoyl}phenyl)- Hz, 2H), 7.43-7.28 (m, 1H), 7.21-7.04 (M + H)⁺ 5-fluoro-1,3- (m, 2H), 6.91-6.81 (m, 2H), 6.81-6.69 (m, dihydro-2H- 1H), 4.77 (d, J = 12.5 Hz, 4H), 3.73 (d, J = isoindole-2- 2.5 Hz, 6H), 3.58-3.39 (m, 2H), 2.93-2.68 carboxamide (m, 2H) 1104 N-(4-{[(2S)-3,3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethyl-1- δ 7.88-7.70 (m, 2H), 7.70-7.57 (m, 2H), m/e 427 (methylamino)-1- 7.45-7.30 (m, 1H), 7.26-7.01 (m, 2H), (M + H)⁺ oxobutan-2- 4.78 (d, J = 12.6 Hz, 4H), 4.41 (d, J = 6.3 yl]carbamoyl}phenyl)- Hz, 1H), 2.64 (s, 3H), 1.03 (s, 9H) 5-fluoro-1,3- dihydro-2H- isoindole-2- carboxamide 1105 N-alpha-(4-{[(5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) fluoro-1,3-dihydro- δ 7.76-7.64 (m, 2H), 7.64-7.54 (m, 2H), m/e 447 2H-isoindol-2- 7.44-7.33 (m, 1H), 7.32-7.22 (m, 4H), (M + H)⁺ yl)carbonyl]amino}benzoyl)-L- 7.25-7.13 (m, 3H), 7.12-6.99 (m, 1H), phenylalaninamide 4.81-4.71 (m, 4H), 4.71-4.61 (m, 1H), 3.20-3.11 (m, 1H), 3.08-2.93 (m, 1H) 1106 N-(4-{[(2R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) amino-4-methyl-1- δ 7.87-7.72 (m, 2H), 7.70-7.52 (m, 2H), m/e 413 oxopentan-2- 7.45-7.26 (m, 1H), 7.24-7.03 (m, 2H), (M + H)⁺ yl]carbamoyl}phenyl)- 4.78 (d, J = 12.6 Hz, 4H), 4.57-4.38 (m, 5-fluoro-1,3- 1H), 1.90-1.47 (m, 3H), 1.07-0.71 (m, dihydro-2H- 6H) isoindole-2- carboxamide 1107 -{4-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyclohexylpiperazin-1- δ 7.76-7.57 (m, 2H), 7.51-7.32 (m, 3H), m/e 451 yl)carbonyl]phenyl}- 7.23-7.03 (m, 2H), 4.77 (d, J = 12.4 Hz, (M + H)⁺ 5-fluoro-1,3-dihydro- 4H), 3.88 (d, J = 76.9 Hz, 4H), 3.22-3.10 2H-isoindole-2- (m, 2H), 2.08 (d, J = 11.3 Hz, 2H), 1.86 (d, J = carboxamide 13.1 Hz, 2H), 1.64 (d, J = 12.9 Hz, 1H), 1.54-1.17 (m, 6H), 1.17-1.04 (m, 1H) 1108 5-fluoro-N-(4-{[3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (methylcarbamoyl)phe- δ 8.16 (t, J = 1.8 Hz, 1H), 7.98-7.80 (m, m/e 433 nyl]carbamoyl}phenyl)- 3H), 7.74-7.59 (m, 2H), 7.59-7.47 (m, (M + H)⁺ 1,3-dihydro-2H- 1H), 7.49-7.33 (m, 2H), 7.24-7.05 (m, isoindole-2- 2H), 4.79 (d, J = 12.5 Hz, 4H), 2.83 (d, J = carboxamide 3.6 Hz, 3H) 1109 N-{4-[(2-amino-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) oxo-1- δ 7.90-7.72 (m, 2H), 7.64 (d, J = 8.7 Hz, m/e 433 phenylethyl)carbamoyl]phenyl}- 2H), 7.50 (d, J = 7.5 Hz, 2H), 7.43-7.26 (M + H)⁺ 5-fluoro- (m, 4H), 7.20-7.02 (m, 2H), 5.62 (s, 1H), 1,3-dihydro-2H- 4.77 (d, J = 12.5 Hz, 4H) isoindole-2- carboxamide 1110 N-{4-[(3-tert- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) butoxypropyl)carbamoyl]phenyl}- δ 7.79-7.66 (m, 2H), 7.66-7.53 (m, 2H), m/e 414 5-fluoro-1,3-dihydro- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.27-7.02 (M + H)⁺ 2H-isoindole-2- (m, 2H), 4.77 (d, J = 12.4 Hz, 4H), 3.44- carboxamide 3.35 (m, 2H), 3.31 (dd, J = 16.4, 9.5 Hz, 2H), 1.73 (p, J = 6.6 Hz, 2H), 1.15 (s, 9H) 1111 N-(4-{[2-(2,6- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethylmorpholin- δ 7.86-7.72 (m, 2H), 7.69-7.55 (m, 2H), m/e 441 4-yl)ethyl]carbamoyl}phenyl)- 7.47-7.32 (m, 1H), 7.24-6.96 (m, 2H), (M + H)⁺ 5-fluoro-1,3- 4.78 (d, J = 12.5 Hz, 4H), 3.92-3.76 (m, dihydro-2H- 2H), 3.67 (t, J = 6.2 Hz, 2H), 3.52 (d, J = isoindole-2- 12.0 Hz, 2H), 3.31 (dd, J = 13.3, 7.0 Hz, carboxamide 3H), 2.71 (t, J = 11.7 Hz, 2H), 1.17 (d, J = 6.3 Hz, 6H) 1112 N-(4-{[(1R)-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) amino-2-oxo-1- δ 7.87-7.70 (m, 2H), 7.70-7.56 (m, 2H), m/e 433 phenylethyl]carbamoyl}phenyl)- 7.51 (dd, J = 11.1, 9.7 Hz, 2H), 7.44-7.25 (M + H)⁺ 5-fluoro- (m, 4H), 7.22-7.00 (m, 2H), 5.62 (s, 1H), 1,3-dihydro-2H- 4.77 (d, J = 12.5 Hz, 4H) isoindole-2- carboxamide- 1113 -fluoro-N-{4-[(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- δ 7.89-7.71 (m, 2H), 7.70-7.53 (m, 2H), m/e 420 1,3-dihydro-2H- 7.43-7.30 (m, 1H), 7.27-7.16 (m, 2H), (M + H)⁺ isoindole-2- 7.16-6.97 (m, 1H), 6.97-6.85 (m, 2H), carboxamide 6.86-6.68 (m, 1H), 4.87-4.65 (m, 4H), 4.54-4.25 (m, 2H), 3.75 (s, 3H) 1114 N-(4-{[2-(3,5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethyl-1H- δ 7.78-7.67 (m, 2H), 7.65-7.52 (m, 2H), m/e 422 pyrazol-1- 7.45-7.29 (m, 1H), 7.25-7.03 (m, 2H), (M + H)⁺ yl)ethyl]carbamoyl}phenyl)- 4.79 (dd, J = 15.9, 8.4 Hz, 4H), 4.16 (t, J = 5-fluoro-1,3- 6.4 Hz, 2H), 3.59 (t, J = 6.4 Hz, 2H), 2.21 (s, dihydro-2H- 3H), 2.14 (s, 3H) isoindole-2- carboxamide 1115 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-2- δ 7.90-7.74 (m, 2H), 7.74-7.56 (m, 2H), m/e 441 (morpholin-4- 7.48-7.31 (m, 1H), 7.28-7.03 (m, 2H), (M + H)⁺ yl)propyl]carbamoyl}phenyl)- 4.78 (d, J = 12.4 Hz, 4H), 4.02-3.80 (m, 1,3-dihydro-2H- 4H), 3.63 (s, 2H), 3.46-3.32 (m, 4H), 1.38 isoindole-2- (s, 6H) carboxamide 1116 5-fluoro-N-(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) {[(3S)-1-methyl-2- δ 7.83-7.70 (m, 2H), 7.68-7.58 (m, 2H), m/e 425 oxoazepan-3- 7.37 (dd, J = 8.3, 5.2 Hz, 1H), 7.24-7.03 (M + H)⁺ yl]carbamoyl}phenyl)- (m, 2H), 4.82-4.69 (m, 5H), 3.65 (dd, J = 1,3-dihydro-2H- 15.6, 11.3 Hz, 1H), 3.03-2.83 (m, 3H), 2.03- isoindole-2- 1.80 (m, 2H), 1.81-1.66 (m, 2H), 1.62- carboxamide 1.33 (m, 2H) 1117 5-fluoro-N-(4-{[2-(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylpiperazin-1- δ 7.81-7.69 (m, 2H), 7.69-7.56 (m, 2H), m/e 426 yl)ethyl]carbamoyl}phenyl)- 7.37 (dd, J = 8.3, 5.2 Hz, 1H), 7.21-6.98 (M + H)⁺ 1,3-dihydro- (m, 2H), 4.77 (d, J = 12.3 Hz, 4H), 3.50 (t, J = 2H-isoindole-2- 6.5 Hz, 2H), 3.25-3.16 (m, 4H), 3.08- carboxamide 2.98 (m, 4H), 2.89 (t, J = 6.5 Hz, 2H), 2.58- 2.46 (m, 3H) 1118 5-fluoro-N-(4-{[4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (morpholin-4- δ 7.87-7.71 (m, 2H), 7.71-7.52 (m, 2H), m/e 474 yl)benzyl]carbamoyl}phenyl)- 7.45-7.29 (m, 1H), 7.19 (dq, J = 9.0, 2.5 (M + H)⁺ 1,3-dihydro-2H- Hz, 3H), 7.14-7.02 (m, 1H), 6.92-6.79 isoindole-2- (m, 2H), 4.77 (d, J = 12.6 Hz, 4H), 4.38 (s, carboxamide 2H), 3.83-3.59 (m, 4H), 3.12-2.95 (m, 4H) 1119 5-fluoro-N-(4-{[3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (piperidin-1- δ 7.84-7.71 (m, 2H), 7.70-7.61 (m, 2H), m/e 425 yl)propyl]carbamoyl}phenyl)- 7.48-7.32 (m, 1H), 7.27-7.01 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 4.77 (d, J = 12.4 Hz, 4H), 3.37 (dd, J = 12.4, isoindole-2- 5.8 Hz, 5H), 3.16-3.01 (m, 3H), 3.01-2.70 carboxamide (m, 2H), 2.07-1.90 (m, 3H), 1.77 (d, J = 46.1 Hz, 6H), 1.46(s, 2H) 1144 5-fluoro-N-{4-[(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxy-2,2- δ 7.76-7.70 (m, 2H), 7.65-7.59 (m, 2H), m/e 400 dimethylpropyl)carbamoyl]phenyl}- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.17 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 9.1, 2.5 Hz, 1H), 7.14-7.05 (m, 1H), 4.79 isoindole-2- (bs, 2H), 4.76 (bs, 2H), 3.15 (s, 2H), 2.99- carboxamide 2.78 (m, 1H), 0.90 (s, 6H) 1145 N-{4-[(3,3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethylbutyl)carbamoyl]phenyl}- δ 7.73 (d, J = 8.6 Hz, 2H), 7.68-7.53 (m, m/e 384 5-fluoro-1,3-dihydro- 2H), 7.48-7.23 (m, 1H), 7.22-7.05 (m, (M + H)⁺ 2H-isoindole-2- 2H), 4.77 (d, J = 12.7 Hz, 4H), 3.29 (dd, J = carboxamide 8.6, 6.6 Hz, 2H), 1.66-1.19 (m, 2H), 0.94 (s, 9H) 1146 5-fluoro-N-(4-{[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (furan-2-yl)propan-2- δ 7.79-7.66 (m, 2H), 7.62-7.49 (m, 2H), m/e 408 yl]carbamoyl}phenyl)- 7.45-7.31 (m, 1H), 7.24-6.96 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 6.51-6.25 (m, 1H), 6.13 (d, J = 3.2 Hz, isoindole-2- 1H), 4.77 (d, J = 12.5 Hz, 4H), 4.27 (h, J = carboxamide 6.7 Hz, 1H), 2.94 (dd, J = 15.0, 6.8 Hz, 2H), 2.87-2.69 (m, 1H), 1.19 (d, J = 6.7 Hz, 3H) 1147 5-fluoro-N-(4-{[(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1,2-oxazol-5- δ 7.86-7.71 (m, 2H), 7.71-7.56 (m, 2H), m/e 395 yl)methyl]carbamoyl}phenyl)- 7.47-7.24 (m, 1H), 7.22-6.98 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 6.16 (s, 1H), 4.88-4.69 (m, 4H), 4.54 (s, isoindole-2- 2H), 2.20 (s, 3H) carboxamide 1148 N-(4-{[(2R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyanobutan-2- δ 7.86-7.72 (m, 2H), 7.72-7.54 (m, 2H), m/e 381 yl]carbamoyl}phenyl)- 7.37 (dd, J = 8.4, 5.2 Hz, 1H), 7.27-7.02 (M + H)⁺ 5-fluoro-1,3- (m, 2H), 4.78 (d, J = 12.4 Hz, 4H), 4.24- dihydro-2H- 4.01 (m, 1H), 2.90-2.65 (m, 2H), 1.76- isoindole-2- 1.53 (m, 2H), 0.92 (t, J = 7.4 Hz, 3H) carboxamide 1149 N-{4-[(2R)-butan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ylcarbamoyl]phenyl}- δ 7.82-7.68 (m, 2H), 7.68-7.52 (m, 2H), m/e 356 5-fluoro-1,3- 7.44-7.27 (m, 1H), 7.26-7.04 (m, 2H), (M + H)⁺ dihydro-2H- 4.77 (d, J = 12.4 Hz, 4H), 4.05-3.76 (m, isoindole-2- 1H), 1.82-1.38 (m, 2H), 1.16 (t, J = 5.3 Hz, carboxamide 3H), 0.88 (t, J = 7.4 Hz, 3H) 1150 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (1H-pyrazol-1- δ 7.78-7.66 (m, 2H), 7.66-7.54 (m, 3H), m/e 394 yl)ethyl]carbamoyl}phenyl)- 7.48-7.27 (m, 2H), 7.24-7.02 (m, 2H), (M + H)⁺ 1,3-dihydro- 4.77 (d, J = 12.5 Hz, 4H), 4.31 (t, J = 6.4 Hz, 2H-isoindole-2- 2H), 3.66 (t, J = 6.4 Hz, 2H), 3.04-2.82 (m, 1H) carboxamide 1151 5-fluoro-N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [methyl(3- δ 7.65-7.50 (m, 2H), 7.37 (d, J = 8.4, 5.2 m/e 384 methylbutyl)carbamoyl]phenyl}- Hz, 1H), 7.32-7.21 (m, 2H), 7.21-7.02 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 4.77 (d, J = 12.6 Hz, 4H), 3.44- isoindole-2- 3.28 (m, 2H), 2.92 (s, 4H), 1.62-1.19 (m, carboxamide 3H), 0.84 (d, J = 6.3 Hz, 6H) 1152 N-(4-{[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (ethylamino)-1- δ 7.87-7.71 (m, 2H), 7.71-7.53 (m, 2H), m/e 399 oxopropan-2- 7.49-7.24 (m, 1H), 7.25-6.98 (m, 2H), (M + H)⁺ yl]carbamoyl}phenyl)- 4.77 (d, J = 12.4 Hz, 4H), 4.55-4.28 (m, 5-fluoro-1,3- 1H), 3.19-3.02 (m, 2H), 3.01-2.74 (m, dihydro-2H- 3H), 1.96 (s, 1H), 1.34 (d, J = 7.1 Hz, 3H), isoindole-2- 1.04 (t, J = 7.2 Hz, 2H) carboxamide 1153 5-fluoro-N-(4-{[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1H-pyrazol-3- δ 7.89-7.69 (m, 2H), 7.69-7.57 (m, 3H), m/e 394 yl)methyl]carbamoyl}phenyl)- 7.50 (d, J = 2.1 Hz, 1H), 7.42-7.22 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 7.25-7.00 (m, 2H), 4.77 (d, J = 12.4 isoindole-2- Hz, 4H), 4.41 (s, 2H), 3.78 (s, 3H), 2.97 (s, carboxamide 2H) 1154 5-fluoro-N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxybutyl)carbamoyl]phenyl}- δ 7.78-7.72 (m, 2H), 7.64-7.58 (m, 2H), m/e 386 1,3-dihydro-2H- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.17 (dd, J = (M + H)⁺ isoindole-2- 9.1, 2.4 Hz, 1H), 7.10 (td, J = 8.9, 2.5 Hz, carboxamide 1H), 4.79 (bs, 3H), 4.76 (bs, 3H), 3.38-3.32 (m, 5H), 3.32 (s, 4H), 1.61-1.39 (m, 2H), 0.90 (t, J = 7.4 Hz, 3H) 1155 N-(4-{[4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (dimethylamino)bu- δ 7.86-7.69 (m, 2H), 7.70-7.54 (m, 2H), m/e 399 tyl]carbamoyl}phenyl)- 7.44-7.27 (m, 1H), 7.23-7.00 (m, 2H), (M + H)⁺ 5-fluoro-1,3- 4.77 (d, J = 12.5 Hz, 4H), 3.31 (dd, J = 13.0, dihydro-2H- 6.3 Hz, 2H), 3.19-2.99 (m, 3H), 2.79 (s, isoindole-2- 7H), 1.71-1.50 (m, 4H) carboxamide 1156 5-fluoro-N-{4-[(3S)- ¹H NMR (400 MHz DMSO-d_(6,) Temp = 90° C.) (ESI(+)) tetrahydrofuran-3- δ 7.82-7.70 (m, 2H), 7.70-7.54 (m, 2H), m/e 370 ylcarbamoyl]phenyl}- 7.44-7.28 (m, 1H), 7.23-7.03 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 4.77 (d, J = 12.5 Hz, 4H), 4.53-4.35 (m, isoindole-2- 1H), 3.98-3.81 (m, 2H), 3.77-3.66 (m, carboxamide 1H), 3.70-3.53 (m, 1H), 3.01-2.87 (m, 1H), 2.32-2.10 (m, 1H), 2.07-1.81 (m, 1H) 1157 5-fluoro-N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxybutan-2- δ 7.78-7.72 (m, 2H), 7.63-7.57 (m, 2H), m/e 386 yl)carbamoyl]phenyl}- 7.40-7.31 (m, 1H), 7.21-7.04 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 4.77 (d, J = 12.4 Hz, 4H), 4.11-3.94 (m, isoindole-2- 1H), 3.55-3.32 (m, 2H), 3.28 (s, 3H), 1.72- carboxamide 1.39 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 1158 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ethoxypropyl)carbamoyl]phenyl}- δ 7.83-7.70 (m, 2H), 7.69-7.51 (m, 2H), m/e 386 5-fluoro-1,3-dihydro- 7.48-7.29 (m, 1H), 7.25-7.00 (m, 2H), (M + H)⁺ 2H-isoindole-2- 4.77 (d, J = 12.5 Hz, 4H), 3.71-3.55 (m, carboxamide 1H), 3.58-3.40 (m, 2H), 3.40-3.29 (m, 1H), 1.26-0.98 (m, 6H) 1159 N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [benzyl(methyl)carbamoyl]phenyl}- δ 7.69-7.53 (m, 2H), 7.42-7.29 (m, 6H), m/e 404 5-fluoro-1,3-dihydro- 7.28 (dd, J = 13.0, 7.2 Hz, 3H), 7.19-7.01 (M + H)⁺ 2H-isoindole-2- (m, 2H), 4.76 (d, J = 12.4 Hz, 4H), 4.58 (d, J = carboxamide 21.5 Hz, 3H), 2.89 (d, J = 3.2 Hz, 3H) 1160 N-{4-[(2S)-butan-2- ¹H NMR (400 MHz, DMSO D₂O) δ 7.83- (ESI(+)) ylcarbamoyl]phenyl}- 7.68 (m, 2H), 7.66-7.54 (m, 2H), 7.37 (dd, m/e 356 5-fluoro-1,3- J = 8.4, 5.2 Hz, 1H), 7.20-7.12 (m, 1H), (M + H)⁺ dihydro-2H- 7.12-7.01 (m, 1H), 4.77 (d, J = 12.5 Hz, isoindole-2- 4H), 3.92 (h, J = 6.6 Hz, 1H), 1.70-1.41 carboxamide (m, 2H), 1.15 (d, J = 6.6 Hz, 3H), 0.88 (t, J = 7.4 Hz, 3H) 1161 5-fluoro-N-(4-{[2-(5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1H-pyrazol- δ 7.83-7.68 (m, 2H), 7.66-7.54 (m, 2H), m/e 408 1-yl)ethyl]carbamoyl}phenyl)- 7.37 (dd, J = 8.4, 5.2 Hz, 1H), 7.20-7.12 (M + H)⁺ 1,3-dihydro- (m, 1H), 7.12-7.01 (m, 1H), 4.77 (d, J = 2H-isoindole-2- 12.5 Hz, 4H), 3.92 (h, J = 6.6 Hz, 4H), 0.88 carboxamide (t, J = 7.4 Hz, 3H) 1162 5-fluoro-N-(4-{[2-(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1H-pyrazol-1- δ 7.77-7.66 (m, 2H), 7.66-7.56 (m, 2H), m/e 408 yl)ethyl]carbamoyl}phenyl)- 7.50 (d, J = 2.1 Hz, 1H), 7.44-7.29 (m, (M + H)⁺ 1,3-dihydro- 1H), 7.17 (dd, J = 9.0, 2.2 Hz, 1H), 7.14- 2H-isoindole-2- 7.00 (m, 1H), 6.00 (d, J = 2.2 Hz, 1H), 4.77 carboxamide (d, J = 12.5 Hz, 4H), 4.21 (t, J = 6.4 Hz, 2H), 3.63 (t, J = 6.4 Hz, 2H), 2.89 (d, J = 62.0 Hz, 1H), 2.21 (d, J = 32.8 Hz, 3H) 1163 5-fluoro-N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylpropyl)carbamoyl]phenyl}- δ 7.82-7.69 (m, 2H), 7.69-7.54 (m, 2H), m/e 356 1,3-dihydro-2H- 7.46-7.26 (m, 1H), 7.29-7.01 (m, 2H), (M + H)⁺ isoindole-2- 4.77 (d, J = 12.4 Hz, 4H), 3.15-3.05 (m, carboxamide 2H), 2.98-2.75 (m, 3H), 2.06-1.89 (m, 2H), 1.92-1.78 (m, 1H), 0.90 (d, J = 6.7 Hz, 7H) 1164 5-fluoro-N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [(pyridin-3- δ 8.79-8.58 (m, 2H), 8.19 (t, J = 7.0 Hz, m/e 391 ylmethyl)carbamoyl] 1H), 7.84-7.73 (m, 2H), 7.73-7.66 (m, (M + H)⁺ phenyl}-1,3-dihydro- 1H), 7.70-7.55 (m, 2H), 7.50-7.27 (m, 2H-isoindole-2- 1H), 7.27-7.06 (m, 2H), 4.77 (d, J = 12.4 carboxamide Hz, 4H), 4.59 (s, 2H) 1165 5-fluoro-N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [(tetrahydrofuran-2- δ 7.85-7.72 (m, 2H), 7.66-7.53 (m, 2H), m/e 384 ylmethyl)carbamoyl] 7.46-7.32 (m, 1H), 7.24-7.14 (m, 1H), (M + H)⁺ phenyl}-1,3-dihydro- 7.14-7.04 (m, 1H), 4.93-4.61 (m, 4H), 2H-isoindole-2- 4.11-3.90 (m, 1H), 3.87-3.72 (m, 1H), carboxamide 3.72-3.53 (m, 1H), 3.35 (t, J = 7.5 Hz, 2H), 2.06-1.73 (m, 3H), 1.66-1.52 (m, 1H) 1166 N-(4-{[(1R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyclopropylethy1]carbamoyl}phenyl)- δ 7.83-7.72 (m, 2H), 7.68-7.57 (m, 2H), m/e 368 5-fluoro-1,3-dihydro- 7.37 (dd, J = 8.3, 5.1 Hz, 1H), 7.23-7.02 (M + H)⁺ 2H-isoindole-2- (m, 2H), 4.77 (d, J = 12.5 Hz, 4H), 3.63- carboxamide 3.42 (m, 1H), 1.22 (d, J = 6.7 Hz, 3H), 1.15- 0.79 (m, 1H), 0.51-0.24 (m, 3H), 0.24- 0.11 (m, 1H) 1167 5-fluoro-N-(4-{[1-(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylcyclopropyl)eth- δ 7.83-7.68 (m, 2H), 7.68-7.54 (m, 2H), m/e 382 yl]carbamoyl}phenyl)- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.24-7.12 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 7.12-7.01 (m, 1H), 4.77 (d, J = isoindole-2- 12.5 Hz, 4H), 3.72 (q, J = 6.8 Hz, 1H), 1.17 carboxamide (d, J = 6.9 Hz, 3H), 1.07 (s, 3H), 0.68-0.51 (m, 1H), 0.49-0.27 (m, 1H), 0.32-0.12 (m, 2H) 1168 5-fluoro-N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [(thiophen-2- δ 7.89-7.70 (m, 2H), 7.70-7.56 (m, 2H), m/e 395 ylmethyl)carbamoyl] 7.48-7.26 (m, 2H), 7.24-7.14 (m, 1H), (M + H)⁺ phenyl}-1,3-dihydro- 7.14-7.05 (m, 1H), 7.05-6.95 (m, 1H), 2H-isoindole-2- 6.98-6.86 (m, 1H), 4.90-4.67 (m, 4H), carboxamide 4.63 (d, J = 4.2 Hz, 2H) 1169 -(4-{[(1S)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyclopropylethyl]carbamoyl}phenyl)- δ 7.85-7.70 (m, 2H), 7.68-7.51 (m, 2H), m/e 368 5-fluoro-1,3-dihydro- 7.37 (dd, J = 8.4, 5.2 Hz, 1H), 7.21-7.05 (M + H)⁺ 2H-isoindole-2- (m, 2H), 4.77 (d, J = 12.4 Hz, 4H), 3.64- carboxamide 3.41 (m, 1H), 1.22 (d, J = 6.7 Hz, 3H), 1.17- 0.94 (m, 1H), 0.51-0.41 (m, 1H), 0.41- 0.34 (m, 1H), 0.34-0.27 (m, 1H), 0.23- 0.11 (m, 1H) 1170 5-fluoro-N-{4-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxybutyl)carbamoyl]phenyl}- δ 7.81-7.67 (m, 2H), 7.67-7.52 (m, 2H), m/e 386 1,3-dihydro-2H- 7.37 (dd, J = 8.3, 5.2 Hz, 1H), 7.17 (d, J = (M + H)⁺ isoindole-2- 9.1 Hz, 1H), 7.14-7.03 (m, 1H), 4.77 (d, J = carboxamide 12.5 Hz, 4H), 3.42-3.30 (m, 2H), 3.24 (s, 3H), 1.96 (s, 1H), 1.70-1.29 (m, 4H) 1171 5-fluoro-N-(4-{[(5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1,3-oxazol-2- δ 7.93-7.72 (m, 2H), 7.69-7.55 (m, 2H), m/e 395 yl)methyl]carbamoyl}phenyl)- 7.45-7.29 (m, 1H), 7.17 (dt, J = 5.5, 2.7 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 7.13-7.04 (m, 1H), 6.72 (dd, J = isoindole-2- 6.4, 1.6 Hz, 1H), 4.77 (d, J = 12.6 Hz, 4H), carboxamide 4.51 (s, 2H), 2.26 (s, 3H) 1172 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (tetrahydro-2H- δ 7.74 (dd, J = 9.0, 2.2 Hz, 2H), 7.61 (dd, J = m/e 412 pyran-3- 9.0, 2.1 Hz, 2H), 7.37 (dd, J = 8.3, 5.2 Hz, (M + H)⁺ yl)ethyl]carbamoyl}phenyl)- 1H), 7.17 (dd, J = 9.0, 2.0 Hz, 1H), 7.14- 1,3-dihydro- 6.99 (m, 1H), 4.77 (d, J = 12.5 Hz, 4H), 3.86- 2H-isoindole-2- 3.57 (m, 2H), 3.38-3.28 (m, 2H), 3.17- carboxamide 2.91 (m, 1H), 1.97-1.73 (m, 1H), 1.74- 1.52 (m, 2H), 1.52-1.34 (m, 3H), 1.33- 1.06 (m, 1H) 1173 5-fluoro-N-(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) {[(2S)-1- δ 7.81-7.72 (m, 2H), 7.69-7.51 (m, 2H), m/e 372 methoxypropan-2- 7.51-7.28 (m, 1H), 7.23-7.14 (m, 1H), (M + H)⁺ yl]carbamoyl}phenyl)- 7.14-6.98 (m, 1H), 4.77 (d, J = 12.5 Hz, 1,3-dihydro-2H- 4H), 4.31-4.10 (m, 1H), 3.44 (dd, J = 9.8, isoindole-2- 6.2 Hz, 1H), 3.35-3.32 (m, 1H), 3.29 (s, carboxamide 3H), 1.16 (d, J = 6.8 Hz, 3H) 1174 N-{4-[(3,3-dimethyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 2-oxobutyl)carbamoyl] δ 7.89-7.70 (m, 2H), 7.70-7.54 (m, 2H), m/e 398 phenyl}-5-fluoro- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.17 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 9.1, 2.2 Hz, 1H), 7.14-6.96 (m, 1H), 4.78 isoindole-2- (d, J = 12.5 Hz, 4H), 4.30 (d, J = 4.1 Hz, carboxamide 2H), 1.18 (s, 9H) 1175 5-fluoro-N-(4-{[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1H-pyrrol-2- δ 7.89-7.70 (m, 2H), 7.70-7.54 (m, 2H), m/e 393 yl)methyl]carbamoyl}phenyl)- 7.37 (dd, J = 8.4, 5.1 Hz, 2H), 7.17 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 9.1, 2.2 Hz, 1H), 7.14-6.96 (m, 1H), 4.78 isoindole-2- (d, J = 12.5 Hz, 4H), 4.30 (d, J = 4.1 Hz, carboxamide 2H), 3.5 (s, 3H) 1176 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (propan-2- δ 7.87-7.68 (m, 2H), 7.68-7.50 (m, 2H), m/e 386 yloxy)ethyl]carbamoyl}phenyl)- 7.37 (dd, J = 8.4, 5.2 Hz, 1H), 7.24-7.15 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 7.15-7.05 (m, 1H), 4.77 (d, J = isoindole-2- 12.5 Hz, 4H), 3.83 (p, J = 6.7 Hz, 1H), 1.88- carboxamide 1.63 (m, 1H), 1.12 (d, J = 6.8 Hz, 3H), 0.90 (dd, J = 6.8, 1.4 Hz, 6H) 1177 N-(4-{[3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (dimethylamino)pro- δ 7.82-7.70 (m, 2H), 7.70-7.55 (m, 2H), m/e 385 pyl]carbamoyl}phenyl)- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.17 (dd, J = (M + H)⁺ 5-fluoro-1,3- 9.0, 2.2 Hz, 1H), 7.15-7.02 (m, 1H), 4.77 dihydro-2H- (d, J = 12.4 Hz, 4H), 3.39-3.30 (m, 2H), isoindole-2- 3.23-3.02 (m, 2H), 2.81 (d, J = 4.3 Hz, carboxamide 6H), 2.02-1.84 (m, 2H) 1178 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) amino-1-oxobutan-2- δ 7.90-7.73 (m, 2H), 7.73-7.50 (m, 2H), m/e 385 yl]carbamoyl}phenyl)- 7.50-7.30 (m, 1H), 7.29-7.13 (m, 1H), (M + H)⁺ 5-fluoro-1,3- 7.13-7.02 (m, 1H), 4.78 (d, J = 12.5 Hz, dihydro-2H- 4H), 4.46-4.31 (m, 1H), 1.96 (s, 1H), 1.91- isoindole-2- 1.78 (m, 1H), 1.78-1.66 (m, 1H), 1.04- carboxamide 0.82 (m, 3H) 1179 5-fluoro-N-[4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (tetrahydro-2H- δ 7.83-7.69 (m, 2H), 7.68-7.54 (m, 2H), m/e 384 pyran-3- 7.42-7.28 (m, 1H), 7.22-7.14 (m, 1H), (M + H)⁺ ylcarbamoyl)phenyl]- 7.14-7.01 (m, 1H), 4.78 (t, J = 10.5 Hz, 1,3-dihydro-2H- 4H), 3.96-3.86 (m, 1H), 3.85-3.70 (m, isoindole-2- 2H), 3.41-3.32 (m, 1H), 2.00-1.88 (m, carboxamide 1H), 1.77-1.65 (m, 1H), 1.65-1.50 (m, 2H) 1180 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (1H-pyrrol-1- δ 7.76-7.66 (m, 2H), 7.66-7.53 (m, 2H), m/e 393 yl)ethyl]carbamoyl}phenyl)- 7.46-7.29 (m, 1H), 7.22-7.13 (m, 1H), (M + H)⁺ 1,3-dihydro- 7.13-6.99 (m, 1H), 6.72 (t, J = 1.9 Hz, 1H), 2H-isoindole-2- 5.99 (t, J = 2.0 Hz, 1H), 4.77 (d, J = 12.5 Hz, carboxamide 4H), 4.07 (t, J = 6.5 Hz, 2H), 3.57 (t, J = 6.5 Hz, 2H) 1181 5-fluoro-N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxypropan-2- δ 7.78-7.72 (m, 2H), 7.64-7.58 (m, 2H), m/e 372 yl)carbamoyl]phenyl}- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.17 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 9.1, 2.4 Hz, 1H), 7.14-7.05 (m, 1H), 4.79 isoindole-2- (bs, 2H), 4.76 (bs, 2H), 4.18 (h, J = 6.5 Hz, carboxamide 1H), 3.44 (dd, J = 9.8, 6.2 Hz, 1H), 2.99- 2.78 (m, 1H), 1.16 (d, J = 6.7 Hz, 3H) 1182 5-fluoro-N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxyethyl)carbamoyl]phenyl}- δ 7.78-7.72 (m, 1H), 7.64-7.56 (m, 1H), m/e 358 1,3-dihydro-2H- 7.41-7.28 (m, 1H), 7.20-7.05 (m, 1H), (M + H)⁺ isoindole-2- 4.78 (bs, 1H), 4.75 (bs, 1H), 3.49 (d, J = 5.2 carboxamide Hz, 1H), 3.48-3.39 (m, 1H), 2.97 (s, 2H), 2.88-2.76 (m, 1H), 1.96 (s, 1H) 1183 N-[4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (cyclopentylcarbamoyl)phenyl]- δ 7.83-7.68 (m, 2H), 7.68-7.53 (m, 2H), m/e 368 5-fluoro- 7.51-7.28 (m, 1H), 7.20-7.13 (m, 1H), (M + H)⁺ 1,3-dihydro-2H- 7.12-7.03 (m, 1H), 4.77 (d, J = 12.4 Hz, isoindole-2- 4H), 4.33-4.12 (m, 1H), 2.00-1.84 (m, carboxamide 2H), 1.82-1.66 (m, 2H), 1.66-1.45 (m, 4H) 1184 5-fluoro-N-(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) {[(2S)-3- δ 7.85-7.69 (m, 2H), 7.66-7.53 (m, 2H), m/e 370 methylbutan-2- 7.46-7.31 (m, 1H), 7.23-7.16 (m, 1H), (M + H)⁺ yl]carbamoyl}phenyl)- 7.16-7.05 (m, 1H), 4.77 (d, J = 12.5 Hz, 1,3-dihydro-2H- 4H), 3.85-3.79 (m, 1H), 1.89-1.72 (m, isoindole-2- 1H), 1.11 (t, J = 5.6 Hz, 3H), 0.90 (dd, J = carboxamide 6.8, 1.1 Hz, 6H) 1185 5-fluoro-N-(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) {[(2R)-3- δ 7.87-7.68 (m, 2H), 7.68-7.50 (m, 2H), m/e 370 methylbutan-2- 7.37 (dd, J = 8.4, 5.2 Hz, 1H), 7.24-7.15 (M + H)⁺ yl]carbamoyl}phenyl)- (m, 1H), 7.15-7.05 (m, 1H), 4.77 (d, J = 1,3-dihydro-2H- 12.5 Hz, 4H), 3.83 (p, J = 6.7 Hz, 1H), 1.88- isoindole-2- 1.63 (m, 1H), 1.12 (d, J = 6.8 Hz, 3H), carboxamide 0.90 (dd, J = 6.8, 1.4 Hz, 6H) 1186 5-fluoro-N-(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) {[(2S)-2- δ 7.84-7.70 (m, 2H), 7.70-7.56 (m, 2H), m/e 370 methylbutyl]carbamoyl}phenyl)- 7.46-7.27 (m, 1H), 7.25-7.03 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 4.77 (d, J = 12.5 Hz, 4H), 3.21 (dd, J = 13.1, isoindole-2- 6.4 Hz, 1H), 3.15-2.97 (m, 1H), 1.80-1.61 carboxamide (m, 1H), 1.53-1.30 (m, 1H), 1.28-1.06 (m, 1H), 0.98-0.79 (m, 6H) 1187 5-fluoro-N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) hydroxy-2- δ 7.81-7.71 (m, 2H), 7.67-7.57 (m, 2H), m/e 372 methylpropyl)carbamoyl]phenyl}- 7.45-7.27 (m, 1H), 7.21-7.13 (m, 1H), (M + H)⁺ 1,3-dihydro-2H- 7.13-7.00 (m, 1H), 4.83-4.70 (m, 4H), isoindole-2- 1.96 (s, 2H), 1.14 (s, 6H) carboxamide 1188 5-fluoro-N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (tetrahydro-2H- δ 7.82-7.67 (m, 2H), 7.69-7.51 (m, 2H), m/e 412 pyran-4- 7.43-7.32 (m, 1H), 7.21-7.01 (m, 2H), (M + H)⁺ yl)ethyl]carbamoyl}phenyl)- 4.78 (t, J = 10.2 Hz, 4H), 3.95-3.70 (m, 1,3-dihydro- 2H), 3.38-3.30 (m, 2H), 1.96 (s, 1H), 1.65- 2H-isoindole-2- 1.55 (m, 2H), 1.57-1.43 (m, 2H), 1.29- carboxamide 1.09 (m, 2H) 1189 N-[4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (butylcarbamoyl)phenyl]- δ 7.81-7.69 (m, 2H), 7.68-7.53 (m, 2H), m/e 356 5-fluoro-1,3- 7.47-7.30 (m, 1H), 7.26-7.13 (m, 1H), (M + H)⁺ dihydro-2H- 7.13-7.01 (m, 1H), 4.87-4.67 (m, 4H), isoindole-2- 3.27 (d, J = 7.1 Hz, 2H), 1.61-1.45 (m, carboxamide 2H), 1.44-1.26 (m, 2H), 0.91 (t, J = 7.3 Hz, 3H) 1190 5-fluoro-N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [methyl(tetrahydrofuran-2- δ 7.69-7.52 (m, 2H), 7.42-7.31 (m, 1H), m/e 398 ylmethyl)carbamoyl] 7.32-7.24 (m, 2H), 7.20-7.14 (m, 1H), (M + H)⁺ phenyl}-1,3-dihydro- 7.14-7.02 (m, 1H), 4.89-4.63 (m, 4H), 2H-isoindole-2- 4.12-3.96 (m, 1H), 3.82-3.58 (m, 2H), carboxamide 3.59-3.34 (m, 2H), 2.00-1.86 (m, 2H), 1.86-1.72 (m, 2H), 1.61-1.33 (m, 1H) 1191 5-fluoro-N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxyethyl)(meth- δ 7.69-7.53 (m, 2H), 7.43-7.32 (m, 1H), m/e 372 yl)carbamoyl]phenyl}- 7.32-7.24 (m, 2H), 7.19-7.13 (m, 1H), (M + H)⁺ 1,3-dihydro-2H- 7.13-7.03 (m, 1H), 4.77 (d, J = 12.4 Hz, isoindole-2- 4H), 3.52 (s, 3H), 3.03-2.92 (m, 3H) carboxamide 1192 N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyanoethyl)carbamoyl]phenyl}- δ 7.89-7.74 (m, 2H), 7.74-7.57 (m, 2H), m/e 353 5-fluoro- 7.37 (dd, J = 8.4, 5.1 Hz, 1H), 7.17 (dd, J = (M + H)⁺ 1,3-dihydro-2H- 9.0, 2.2 Hz, 1H), 7.13-7.04 (m, 1H), 4.93 isoindole-2- (q, J = 7.2 Hz, 1H), 4.78 (d, J = 12.4 Hz, carboxamide 4H), 1.57 (d, J = 7.2 Hz, 3H) 1193 5-fluoro-N-(4-{[(5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-1,2-oxazol-3- δ 7.85-7.72 (m, 2H), 7.68-7.56 (m, 2H), m/e 395 yl)methyl]carbamoyl}phenyl)- 7.42-7.28 (m, 1H), 7.21-7.12 (m, 1H), (M + H)⁺ 1,3-dihydro-2H- 7.12-7.01 (m, 1H), 6.24-6.00 (m, 1H), isoindole-2- 4.90-4.68 (m, 4H), 4.55-4.37 (m, 2H), carboxamide 2.42-2.27 (m, 3H) 1194 5-fluoro-N-{4-[(3R)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) tetrahydrofuran-3- δ 7.87-7.72 (m, 2H), 7.66-7.55 (m, 2H), m/e 370 ylcarbamoyl]phenyl}- 7.45-7.32 (m, 1H), 7.17 (dd, J = 9.0, 2.1 (M + H)⁺ 1,3-dihydro-2H- Hz, 1H), 7.14-7.01 (m, 1H), 4.77 (d, J = isoindole-2- 12.4 Hz, 4H), 4.50-4.38 (m, 1H), 3.93- carboxamide 3.80 (m, 2H), 3.80-3.66 (m, 1H), 3.59 (dd, J = 8.9, 4.6 Hz, 1H), 2.27-2.09 (m, 1H), 1.99-1.77 (m, 1H) 1260 N-{4-[(3-methoxy-2,2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethylpropyl)carbamoyl]phenyl}- δ 7.80-7.70 (m, 2H), 7.68-7.52 (m, 2H), m/e 382 1,3-dihydro-2H- 7.44-7.23 (m, 4H), 4.79 (s, 4H), 3.29 (d, J = (M + H)⁺ isoindole-2- 7.7 Hz, 3H), 3.22-3.19 (m, 2H), 3.15 (s, carboxamide 2H), 0.90 (s, 6H) 1261 N-{4-[(4,4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) difluorocyclohexyl)carbamoyl]phenyl}- δ 7.86-7.69 (m, 2H), 7.69-7.50 (m, 2H), m/e 382 1,3-dihydro-2H- 7.38-7.22 (m, 4H), 4.99-4.62 (m, 4H), (M + H)⁺ isoindole-2- 3.96 (s, 1H), 2.20-1.82 (m, 6H), 1.70 (t, J = carboxamide 11.7 Hz, 2H) 1262 N-(4-{[(2R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyanobutan-2- δ 7.87-7.70 (m, 2H), 7.73-7.49 (m, 2H), m/e 362 yl]carbamoyl}phenyl)- 7.45-7.17 (m, 4H), 4.80 (s, 4H), 4.23-3.99 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 2.97-2.63 (m, 2H), 1.78-1.56 (m, isoindole-2- 2H), 0.91 (q, J = 7.2 Hz, 3H) carboxamide 1263 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxybutyl)carbamoyl]phenyl}- δ 7.77-7.70 (m, 2H), 7.69-7.52 (m, 2H), m/e 368 1,3-dihydro-2H- 7.42-7.22 (m, 4H), 4.79 (s, 4H), 3.41-3.31 (M + H)⁺ isoindole-2- (m, 5H), 1.65-1.30 (m, 2H), 0.90 (t, J = 7.4 carboxamide Hz, 3H) 1264 N-(4-{[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (ethylamino)-1- δ 7.88-7.73 (m, 2H), 7.69-7.55 (m, 2H), m/e 381 oxopropan-2- 7.48-7.16 (m, 4H), 4.80 (s, 4H), 4.58-4.35 (M + H)⁺ yl]carbamoyl}phenyl)- (m, 1H), 3.13 (q, J = 7.2 Hz, 2H), 1.35 (d, J = 1,3-dihydro-2H- 7.2 Hz, 3H), 1.05 (t, J = 7.2 Hz, 3H) isoindole-2- carboxamide 1265 N-(4-{[2-methyl-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (morpholin-4- δ 7.95-7.77 (m, 2H), 7.70 (t, J = 10.6 Hz, m/e 437 yl)butyl]carbamoyl} 2H), 7.48-7.20 (m, 4H), 4.80 (s, 4H), 3.95 (M + H)⁺ phenyl)-1,3-dihydro- (d, J = 20.8 Hz, 4H), 3.75-3.55 (m, 2H), 2H-isoindole-2- 3.40 (s, 2H), 1.95-1.63 (m, 2H), 1.34 (s, carboxamide 3H), 1.02 (t, J = 7.4 Hz, 3H) 1266 N-(4-{[(1R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyclopropylethy1]carbamoyl}phenyl)- δ 7.86-7.69 (m, 2H), 7.69-7.53 (m, 2H), m/e 350 1,3-dihydro-2H- 7.49-7.13 (m, 4H), 4.79 (s, 4H), 3.63-3.44 (M + H)⁺ isoindole-2- (m, 1H), 1.22 (d, J = 6.7 Hz, 3H), 1.09- carboxamide 0.90 (m, 1H), 0.57-0.12 (m, 4H) 1267 N-(4-{[(1S)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) cyclopropylethy1]carbamoyl}phenyl)- δ 7.84-7.71 (m, 2H), 7.66-7.55 (m, 2H), m/e 350 1,3-dihydro-2H- 7.40-7.19 (m, 4H), 4.79 (s, 4H), 3.52 (p, J = (M + H)⁺ isoindole-2- 6.9 Hz, 1H), 1.22 (d, J = 6.7 Hz, 3H), 1.13- carboxamide 0.90 (m, 1H), 0.54-0.14 (m, 4H) 1269 N-{4-[(3S)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) tetrahydrofuran-3- δ 7.84-7.73 (m, 2H), 7.67-7.53 (m, 2H), m/e 351 ylcarbamoyl]phenyl}- 7.42-7.19 (m, 4H), 4.80 (d, J = 5.5 Hz, (M + H)⁺ 1,3-dihydro-2H- 4H), 4.52-4.35 (m, 1H), 3.93-3.78 (m, isoindole-2- 2H), 3.78-3.67 (m, 1H), 3.63-3.52 (m, carboxamide 1H), 2.29-2.08 (m, 1H), 2.07-1.79 (m, 1H) 1270 N-(4-{[2-(tetrahydro- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 2H-pyran-3- δ 7.82-7.69 (m, 2H), 7.65-7.48 (m, 2H), m/e 394 yl)ethyl]carbamoyl}phenyl)- 7.50-7.14 (m, 4H), 4.79 (s, 4H), 3.93-3.60 (M + H)⁺ 1,3-dihydro- (m, 2H), 3.41-3.29 (m, 2H), 3.14-2.93 (m, 2H-isoindole-2- 1H), 2.02-1.79 (m, 1H), 1.69-1.43 (m, carboxamide 4H), 1.29-1.09 (m, 1H) 1271 N-(4-{[(5-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 1,3-oxazol-2- δ 7.92-7.71 (m, 2H), 7.72-7.56 (m, 2H), m/e 377 yl)methyl]carbamoyl}phenyl)- 7.46-7.24 (m, 4H), 4.80 (d, J = 1.4 Hz, (M + H)⁺ 1,3-dihydro-2H- 4H), 4.63-4.41 (m, 2H), 2.26 (t, J = 2.3 Hz, 3H) isoindole-2- carboxamide 1272 N-[4-({2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [(dimethylamino)meth- δ 7.85-7.75 (m, 2H), 7.72-7.63 (m, 2H), m/e 429 yl]benzyl}carbamoyl)phenyl]- 7.59-7.50 (m, 1H), 7.50-7.42 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.42-7.24 (m, 5H), 4.79 (s, 4H), 4.52 (d, J = isoindole-2- 16.7 Hz, 4H), 2.88 (s, 6H) carboxamide 1273 N-(4-{[(1R)-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) amino-2-oxo-1- δ 7.86-7.76 (m, 2H), 7.70-7.62 (m, 2H), m/e 415 phenylethyl]carbamoyl}phenyl)- 7.51 (t, J = 6.8 Hz, 2H), 7.40-7.25 (m, 7H), (M + H)⁺ 1,3-dihydro-2H- 5.63 (s, 1H), 4.79 (s, 4H) isoindole-2- carboxamide 1274 N-[4-(1,3-oxazol-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ylcarbamoyl)phenyl]- δ 8.03-7.85 (m, 2H), 7.85-7.76 (m, 1H), m/e 329 1,3-dihydro-2H- 7.76-7.61 (m, 2H), 7.47-7.25 (m, 4H), (M + H)⁺ isoindole-2- 7.18-7.03 (m, 1H), 4.92-4.62 (m, 4H) carboxamide 1275 N-[4-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) pyran-3- δ 7.88-7.65 (m, 2H), 7.69-7.53 (m, 2H), m/e 366 ylcarbamoyl)phenyl]- 7.46-7.18 (m, 4H), 4.79 (s, 4H), 3.99-3.66 (M + H)⁺ 1,3-dihydro-2H- (m, 3H), 3.44-3.32 (m, 1H), 2.04-1.86 (m, isoindole-2- 1H), 1.84-1.50 (m, 3H) carboxamide 1276 N-(4-{[2-(2,6- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethylmorpholin- δ 7.85-7.70 (m, 2H), 7.70-7.57 (m, 2H), m/e 423 4-yl)ethyl]carbamoyl}phenyl)- 7.45-7.22 (m, 4H), 4.80 (s, 4H), 3.94-3.77 (M + H)⁺ 1,3-dihydro- (m, 2H), 3.67 (t, J = 6.2 Hz, 2H), 3.53 (d, J = 2H-isoindole-2- 12.0 Hz, 2H), 3.32 (dd, J = 12.8, 6.6 Hz, carboxamide 3H), 2.72 (t, J = 11.7 Hz, 2H), 1.18 (d, J = 6.3 Hz, 6H) 1277 N-(4-{[1-(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylcyclopropyl)eth- δ 7.85-7.69 (m, 2H), 7.69-7.53 (m, 2H), m/e 364 yl]carbamoyl}phenyl)- 7.47-6.99 (m, 4H), 4.79 (s, 4H), 3.82-3.62 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 1.17 (d, J = 6.9 Hz, 3H), 1.07 (s, isoindole-2- 3H), 0.69-0.53 (m, 1H), 0.47-0.35 (m, carboxamide 1H), 0.29-0.13 (m, 2H) 1278 N-(4-{[2-(furan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) yl)-2-(pyrrolidin-1- δ 7.79-7.65 (m, 3H), 7.68-7.54 (m, 2H), m/e 445 yl)ethyl]carbamoyl}phenyl)- 7.43-7.17 (m, 4H), 6.78 (d, J = 3.3 Hz, (M + H)⁺ 1,3-dihydro- 1H), 6.64-6.46 (m, 1H), 4.91-4.72 (m, 2H-isoindole-2- 5H), 4.11-3.93 (m, 1H), 3.93-3.77 (m, carboxamide 1H), 2.01-1.76 (m, 4H) 1310 N-(4-{[3-(3,5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethyl-1H- δ 7.80-7.69 (m, 2H), 7.69-7.51 (m, 2H), m/e 418 pyrazol-1- 7.44-7.25 (m, 4H), 4.79 (s, 4H), 4.03-3.87 (M + H)⁺ yl)propyl]carbamoyl}phenyl)- (m, 2H), 2.23-2.15 (m, 3H), 2.10 (s, 3H), 1,3-dihydro-2H- 2.05-1.88 (m, 2H) isoindole-2- carboxamide 1311 N-(4-{[(3S)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methyl-2-oxoazepan-3- δ 7.92-7.83 (m, 1H), 7.79-7.70 (m, 2H), m/e 407 yl]carbamoyl}phenyl)- 7.70-7.57 (m, 2H), 7.46-7.13 (m, 5H), (M + H)⁺ 1,3-dihydro-2H- 6.63-6.61 (m, 1H), 4.90-4.73 (m, 6H), isoindole-2- 3.76-3.57 (m, 1H), 2.95 (s, 3H), 2.02-1.68 carboxamide (m, 4H), 1.64-1.32 (m, 2H) 1312 N-(4-{[2-(1H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) pyrazol-1- δ 7.74-7.67 (m, 2H), 7.66-7.59 (m, 3H), m/e 376 yl)ethyl]carbamoyl}phenyl)- 7.39-7.28 (m, 4H), 6.23 (t, J = 2.0 Hz, 1H), (M + H)⁺ 1,3-dihydro- 4.79 (s, 4H), 4.31 (t, J = 6.4 Hz, 2H), 3.66 (t, 2H-isoindole-2- J = 6.4 Hz, 2H) carboxamide 1313 N-(4-{[1-(1,3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) thiazol-2- δ 7.91-7.75 (m, 2H), 7.74-7.62 (m, 3H), m/e 393 yl)ethyl]carbamoyl}phenyl)- 7.53 (d, J = 3.3 Hz, 1H), 7.47-7.23 (m, (M + H)⁺ 1,3-dihydro- 4H), 5.56-5.34 (m, 1H), 4.80 (s, 4H), 1.65 2H-isoindole-2- (d, J = 7.0 Hz, 3H) carboxamide 1314 N-(4-{[1-(furan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) yl)propan-2- δ 7.77-7.66 (m, 2H), 7.66-7.55 (m, 2H), m/e 390 yl]carbamoyl}phenyl)- 7.50-7.39 (m, 1H), 7.41-7.19 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 6.45-6.23 (m, 1H), 6.13 (d, J = 3.1 Hz, isoindole-2- 1H), 4.79 (s, 4H), 4.39-4.14 (m, 1H), 3.03- carboxamide 2.87 (m, 1H), 2.87-2.70 (m, 1H), 1.19 (d, J = 6.7 Hz, 3H) 1315 N-(4-{[1-(1-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 1H-pyrazol-4- δ 7.81-7.68 (m, 2H), 7.70-7.57 (m, 2H), m/e 390 yl)ethyl]carbamoyl}phenyl)- 7.54 (s, 1H), 7.47-7.20 (m, 4H), 5.14 (q, J = (M + H)⁺ 1,3-dihydro- 6.9 Hz, 1H), 4.79 (s, 4H), 3.78 (s, 3H), 2H-isoindole-2- 1.47 (d, J = 6.9 Hz, 3H) carboxamide 1316 N-(4-{[(2R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) amino-4-methyl-1- δ 7.93-7.76 (m, 2H), 7.76-7.52 (m, 2H), m/e 395 oxopentan-2- 7.46-7.19 (m, 4H), 4.80 (s, 4H), 4.62-4.39 (M + H)⁺ yl]carbamoyl}phenyl)- (m, 1H), 1.78-1.50 (m, 3H), 0.92 (dd, J = 1,3-dihydro-2H- 11.0, 6.1 Hz, 6H) isoindole-2- carboxamide 1317 N-(4-{[1-(3,5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethyl-1H- δ 7.80-7.67 (m, 2H), 7.66-7.56 (m, 2H), m/e 418 pyrazol-1-yl)propan-2- 7.48-7.09 (m, 4H), 4.79 (s, 4H), 4.38 (h, J = (M + H)⁺ yl]carbamoyl}phenyl)- 6.6 Hz, 1H), 4.22-4.00 (m, 2H), 2.25 (s, 1,3-dihydro-2H- 3H), 2.14 (s, 3H), 1.16 (d, J = 6.8 Hz, 3H) isoindole-2- carboxamide 1318 N-{4-[(2,2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) difluoroethyl)carbamoyl]phenyl}- δ 7.93-7.72 (m, 2H), 7.73-7.57 (m, 2H), m/e 346 1,3-dihydro-2H- 7.44-7.22 (m, 4H), 6.28-5.80 (m, 1H), (M + H)⁺ isoindole-2- 4.79 (s, 4H), 3.78-3.55 (m, 2H) carboxamide 1319 N-(4-{[2-(tetrahydro- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 2H-pyran-4- δ 7.81-7.68 (m, 2H), 7.68-7.53 (m, 2H), m/e 394 yl)ethyl]carbamoyl}phenyl)- 7.44-7.25 (m, 4H), 4.79 (s, 4H), 3.93-3.74 (M + H)⁺ 1,3-dihydro- (m, 2H), 3.34-3.30 (m, 2H), 1.73-1.43 (m, 2H-isoindole-2- 4H), 1.35-1.06 (m, 2H) carboxamide 1320 N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) [(tetrahydrofuran-2- δ 7.83-7.72 (m, 2H), 7.67-7.47 (m, 2H), m/e 366 ylmethyl)carbamoyl] 7.43-7.17 (m, 4H), 4.79 (s, 4H), 4.00 (p, J = (M + H)⁺ phenyl}-1,3-dihydro- 6.2 Hz, 1H), 3.88-3.72 (m, 1H), 3.73- 2H-isoindole-2- 3.55 (m, 1H), 3.34 (d, J = 5.9 Hz, 2H), 2.01- carboxamide 1.76 (m, 3H), 1.71-1.49 (m, 1H) 1321 N-{4-[(2-methoxy-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylpropyl)carbamoyl]phenyl}- δ 7.86-7.71 (m, 2H), 7.71-7.58 (m, 2H), m/e 368 1,3-dihydro-2H- 7.46-7.22 (m, 4H), 4.79 (s, 4H), 3.35 (s, (M + H)⁺ isoindole-2- 2H), 3.18 (s, 3H), 1.14 (s, 6H) carboxamide 1322 N-(4-{[(5-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) l,2-oxazol-3- δ 7.81-7.75 (m, 2H), 7.67-7.61 (m, 2H), m/e 377 yl)methyl]carbamoyl}phenyl)- 7.39-7.28 (m, 4H), 4.83-4.76 (m, 5H), (M + H)⁺ 1,3-dihydro-2H- 4.46 (s, 2H), 2.36 (d, J = 0.9 Hz, 3H) isoindole-2- carboxamide 1323 N-(4-{[(1-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 1H-pyrazol-4- δ 7.75 (d, J = 8.7 Hz, 2H), 7.62 (d, J = 8.7 m/e 376 yl)methyl]carbamoyl}phenyl)- Hz, 2H), 7.54 (s, 1H), 7.39-7.20 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 4.79 (s, 4H), 4.30 (s, 2H), 3.78 (s, 3H) isoindole-2- carboxamide 1324 N-(4-{[2-(3,5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethyl-1H- δ 7.83-7.64 (m, 2H), 7.68-7.53 (m, 2H), m/e 404 pyrazol-1- 7.46-7.13 (m, 4H), 4.79 (s, 4H), 4.13 (t, J = (M + H)⁺ yl)ethyl]carbamoyl}phenyl)- 6.5 Hz, 2H), 3.58 (t, J = 6.5 Hz, 2H), 2.19 (s, 1,3-dihydro- 3H), 2.12 (s, 3H) 2H-isoindole-2- carboxamide 1325 N-alpha-{4-[(1,3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dihydro-2H-isoindol-2- δ 7.70-7.66 (m, 2H), 7.66-7.56 (m, 2H), m/e 429 ylcarbonyl)amino]benzoyl}-L- 7.39-7.22 (m, 8H), 7.22-7.12 (m, 1H), (M + H)⁺ phenylalaninamide 4.79 (s, 4H), 4.72-4.62 (m, 1H), 3.20-3.11 (m, 1H), 3.08-2.91 (m, 1H) 1326 N-(4-{[2-(2-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 1,3-thiazol-4- δ 7.74 (dd, J = 6.8, 1.8 Hz, 2H), 7.70-7.57 m/e 477 yl)ethyl]carbamoyl}phenyl)- (m, 2H), 7.43-7.23 (m, 4H), 7.19-6.98 (m, (M + H)⁺ 1,3-dihydro- 1H), 4.80 (s, 4H), 3.66-3.41 (m, 2H), 3.05- 2H-isoindole-2- 2.85 (m, 2H), 2.65 (d, J = 5.2 Hz, 3H) carboxamide 1327 N-(4-{[(2S)-3,3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) dimethyl-1- δ 7.87-7.69 (m, 2H), 7.69-7.49 (m, 2H), m/e 409 (methylamino)-1- 7.49-7.24 (m, 4H), 4.80 (s, 4H), 4.45-4.33 (M + H)⁺ oxobutan-2- (m, 1H), 2.66 (d, J = 20.0 Hz, 3H), 1.02 (d, J = yl]carbamoyl}phenyl)- 18.5 Hz, 9H) 1,3-dihydro-2H- isoindole-2- carboxamide 1328 N-[4-(thiophen-3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ylcarbamoyl)phenyl]- δ 7.97-7.82 (m, 2H), 7.75-7.61 (m, 3H), m/e 364 1,3-dihydro-2H- 7.46-7.24 (m, 5H), 4.81 (s, 4H) (M + H)⁺ isoindole-2- carboxamide 1329 N-(4-{[2-(5-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 1H-pyrazol-1- δ 7.80-7.67 (m, 2H), 7.67-7.55 (m, 2H), m/e 390 yl)ethyl]carbamoyl}phenyl)- 7.45-7.20 (m, 5H), 6.00 (dd, J = 5.0, 0.7 (M + H)⁺ 1,3-dihydro- Hz, 1H), 4.79 (s, 4H), 4.21 (t, J = 6.6 Hz, 2H-isoindole-2- 2H), 3.61 (t, J = 6.6 Hz, 2H), 2.25 (s, 3H) carboxamide 1330 N-(4-{[2-(3-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 1H-pyrazol-1- δ 7.76-7.68 (m, 2H), 7.68-7.52 (m, 2H), m/e 390 yl)ethyl]carbamoyl}phenyl)- 7.56-7.42 (m, 1H), 7.44-7.24 (m, 4H), (M + H)⁺ 1,3-dihydro- 5.99 (d, J = 2.1 Hz, 1H), 4.79 (s, 4H), 4.21 2H-isoindole-2- (t, J = 6.4 Hz, 2H), 3.63 (t, J = 6.4 Hz, 2H), carboxamide 2.21 (d, J = 33.1 Hz, 3H) 1331 N-{4-[(2S)-butan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ylcarbamoyl]phenyl}- δ 7.88-7.68 (m, 2H), 7.66-7.49 (m, 2H), m/e 338 1,3-dihydro-2H- 7.44-7.19 (m, 4H), 4.79 (s, 4H), 4.01-3.80 (M + H)⁺ isoindole-2- (m, 1H), 1.70-1.33 (m, 2H), 1.16 (d, J = 6.6 carboxamide Hz, 3H), 0.88 (t, J = 7.4 Hz, 3H) 1332 N-{4-[(3,3-dimethyl-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) oxobutyl)carbamoyl] δ 7.88-7.69 (m, 2H), 7.72-7.54 (m, 2H), m/e 380 phenyl}-1,3-dihydro- 7.47-7.19 (m, 4H), 4.80 (s, 4H), 4.30 (s, (M + H)⁺ 2H-isoindole-2- 2H), 1.18 (s, 9H) carboxamide 1333 N-(4-{[(1-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) 1H-pyrazol-3- δ 7.83-7.73 (m, 2H), 7.70-7.59 (m, 2H), m/e 376 yl)methyl]carbamoyl}phenyl)- 7.55-7.46 (m, 1H), 7.41-7.22 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 6.15 (d, J = 2.2 Hz, 1H), 4.79 (s, 4H), 4.42 isoindole-2- (s, 2H) carboxamide 1334 N-(4-{[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (acetylamino)phenyl] δ 7.90-7.79 (m, 2H), 7.76-7.66 (m, 3H), m/e 415 carbamoyl}phenyl)- 7.51-7.42 (m, 1H), 7.41-7.26 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 7.26-7.13 (m, 2H), 4.85-4.77 (m, 4H), isoindole-2- 2.14-2.05 (m, 3H) carboxamide 1335 N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methoxybutan-2- δ 7.83-7.70 (m, 2H), 7.70-7.55 (m, 2H), m/e 368 yl)carbamoyl]phenyl}- 7.45-7.23 (m, 4H), 4.79 (s, 4H), 4.16-3.89 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 3.52-3.33 (m, 2H), 1.75-1.42 (m, isoindole-2- 2H), 0.90 (t, J = 7.4 Hz, 3H) carboxamide 1336 N-[4-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) pyran-4- δ 7.85-7.71 (m, 2H), 7.66-7.53 (m, 2H), m/e 366 ylcarbamoyl)phenyl]- 7.48-7.20 (m, 4H), 4.79 (s, 4H), 4.05-3.82 (M + H)⁺ 1,3-dihydro-2H- (m, 3H), 3.48-3.31 (m, 2H), 1.93-1.70 (m, isoindole-2- 2H), 1.70-1.48 (m, 2H) carboxamide 1337 N-[4-(pyrimidin-4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ylcarbamoyl)phenyl]- δ 8.93-8.85 (m, 1H), 8.72-8.62 (m, 1H), m/e 359 1,3-dihydro-2H- 8.21-8.11 (m, 1H), 8.03-7.91 (m, 2H), (M + H)⁺ isoindole-2- 7.77-7.66 (m, 2H), 7.42-7.26 (m, 4H), carboxamide 4.81 (d, J = 5.2 Hz, 4H) 1338 N-(4-{[2-(1H-pyrrol-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) yl)ethyl]carbamoyl}phenyl)- δ 7.78-7.66 (m, 2H), 7.66-7.57 (m, 2H), m/e 375 1,3-dihydro- 7.37-7.26 (m, 4H), 6.87-6.56 (m, 1H), (M + H)⁺ 2H-isoindole-2- 6.10-5.80 (m, 1H), 4.79 (s, 4H), 4.08 (t, J = carboxamide 6.5 Hz, 2H), 3.70-3.48 (m, 2H) 1339 N-(4-{[(2S)-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylbutyl]carbamoyl}phenyl)- δ 7.83-7.70 (m, 2H), 7.70-7.52 (m, 2H), m/e 352 1,3-dihydro-2H- 7.45-7.17 (m, 4H), 4.79 (s, 4H), 3.24-3.16 (M + H)⁺ isoindole-2- (m, 1H), 3.16-2.98 (m, 1H), 1.77-1.55 (m, carboxamide 1H), 1.51-1.31 (m, 1H), 1.31-1.01 (m, 1H), 0.90 (dd, J = 13.5, 6.4 Hz, 6H) 1340 N-{4-[(1-amino-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) oxohexan-2- δ 7.86-7.70 (m, 3H), 7.68-7.47 (m, 3H), m/e 395 yl)carbamoyl]phenyl}- 7.47-6.53 (m, 6H), 4.84-4.32 (m, 7H), (M + H)⁺ 1,3-dihydro-2H- 3.27 (s, 73H), 2.61-2.29 (m, 1 1H), 2.04- isoindole-2- 1.61 (m, 3H), 1.56-0.69 (m, 10H), 0.18-−0.03 carboxamide (m, 2H) 1341 N-{4-[(2-amino-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) oxo-1- δ 7.86-7.73 (m, 2H), 7.84-7.78 (m, 2H), m/e 3 15 phenylethyl)carbamoyl]phenyl}- 7.70-7.57 (m, 2H), 7.68-7.62 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 7.53-7.49 (m, 1H), 7.51 (dd, J = 6.8, 5.5 isoindole-2- Hz, 2H), 7.40-7.26 (m, 7H), 7.36-7.22 carboxamide (m, 5H), 5.63 (s, 1H), 5.63 (s, 1H), 4.79 (s, 4H), 4.79 (s, 4H) 1342 N-{4-[(3-tert- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) butoxypropyl)carbamoyl]phenyl}- δ 7.80-7.68 (m, 2H), 7.68-7.53 (m, 2H), m/e 396 1,3-dihydro-2H- 7.37-7.18 (m, 4H), 4.79 (s, 4H), 3.44-3.29 (M + H)⁺ isoindole-2- (m, 4H), 1.81-1.62 (m, 2H), 1.15 (s, 9H) carboxamide 1343 N-(4-{[3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (methylcarbamoyl)phe- δ 7.97-7.85 (m, 3H), 7.76-7.65 (m, 2H), m/e 415 nyl]carbamoyl}phenyl)- 7.45-7.26 (m, 6H), 4.85-4.77 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 2.86-2.78 (m, 3H) isoindole-2- carboxamide 1344 N-(4-{[(2R)-3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylbutan-2- δ 7.90-7.68 (m, 2H), 7.66-7.56 (m, 2H), m/e 352 yl]carbamoyl}phenyl)- 7.40-7.17 (m, 4H), 4.79 (s, 4H), 4.02-3.72 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 1.94-1.65 (m, 1H), 1.12 (d, J = 6.7 isoindole-2- Hz, 3H), 0.90 (d, J = 6.8 Hz, 6H) carboxamide 1345 N-(4-{[(2S)-3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) methylbutan-2- δ 7.85-7.68 (m, 2H), 7.67-7.51 (m, 2H), m/e 352 yl]carbamoyl}phenyl)- 7.48-7.11 (m, 4H), 4.79 (s, 4H), 3.95-3.74 (M + H)⁺ 1,3-dihydro-2H- (m, 1H), 1.92-1.64 (m, 1H), 1.12 (d, J = 6.8 isoindole-2- Hz, 3H), 1.00-0.79 (m, 6H) carboxamide 1346 N-(4-{[2-methyl-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (morpholin-4- δ 7.83-7.70 (m, 2H), 7.70-7.52 (m, 2H), m/e 423 yl)propan-2- 7.45-7.17 (m, 4H), 4.79 (s, 4H), 3.24-3.16 (M + H)⁺ yl]carbamoyl}phenyl)- (m, 1H), 3.16-2.98 (m, 1H), 1.77-1.55 (m, 1,3-dihydro-2H- 1H), 1.51-1.31 (m, 1H), 1.31-1.01 (m, isoindole-2- 1H), 0.90 (dd, J = 13.5, 6.4 Hz, 6H) carboxamide 1348 N-(4-{[2-methyl-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) (morpholin-4- δ 7.91-7.75 (m, 2H), 7.75-7.60 (m, 2H), m/e 423 yl)propyl]carbamoyl}phenyl)- 7.44-7.23 (m, 4H), 4.80 (s, 4H), 4.01-3.86 (M + H)⁺ 1,3-dihydro-2H- (m, 4H), 3.63 (s, 2H), 3.50-3.35 (m, 4H), isoindole-2- 1.38 (s, 6H) carboxamide 1349 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) (ESI(+)) ethoxypropyl)carbamoyl]phenyl}- δ 7.84-7.70 (m, 2H), 7.70-7.55 (m, 2H), m/e 368 1,3-dihydro-2H- 7.43-7.24 (m, 4H), 4.79 (s, 4H), 3.72-3.55 (M + H)⁺ isoindole-2- (m, 1H), 3.58-3.44 (m, 2H), 3.38-3.31 (m, carboxamide 1H), 1.20-1.01 (m, 6H)

Example 132 N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide

A solution of 5-cyano-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide (30 mg, 0.9 mmol) in sulfuric acid (0.1 mL) and trifluoroacetic acid (0.3 mL) was stirred at room temperature for 16 hours. The reaction was treated with ice and the suspension was stirred for 10 minutes and filtered. The solid collected was washed with water and dried under vacuum; the solid was purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), 8.26 (t, J=5.7 Hz, 1H), 7.97-8.00 (bs, 1H), 7.81-7.86 (m, 2H), 7.75-7.79 (m, 2H), 7.63-7.68 (m, 2H), 7.44 (d, J=7.8 Hz, 1H), 7.34-7.39 (bs, 1H), 4.81-4.82 (bs, 4H), 3.16-3.24 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 367 (M+H)⁺.

Example 272 methyl 2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate Example 272A 4-amino-N-propylbenzamide 5-amino-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

A solution of 4-nitro-N-propylbenzamide (800 mg, 0.1 mmol) in 40 ml tetrahydrofuran in the presence of 160 mg of 20% Pd on carbon was treated in a pressure bottle with 30 psi of hydrogen for 30 minutes at room temperature. The suspension was filtered through a nylon membrane and concentrated to provide the title compound.

Example 272B methyl 2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate

A solution of 4-amino-N-propylbenzamide (390 mg, 2.19 mmol), bis(2,5-dioxopyrrolidin-1-yl) carbonate (700 mg, 2.74 mmol), and pyridine (0.18 mL, 2.19 mmol) in acetonitrile (5 mL) was stirred at ambient temperature for 30 minutes. Diisopropylethylamine (0.85 mL, 6.6 mmol)) was added followed by a suspension of methyl isoindoline-5-carboxylate hydrochloride (538 mg, 2.52 mmol) and diisopropylethylamine (0.46 mL, 4.4 mmol) in 1-methyl-2-pyrrolidinone (8 mL) added dropwise via syringe over 5 minutes. The reaction became a suspension and was stirred 3 hours. The reaction was treated with water (30 mL) and the resulting suspension was stirred 5 minutes and filtered. The solid collected was washed with water and dried under vacuum to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.63 (s, 1H), 8.26 (t, J=5.6 Hz, 1H), 7.94-7.97 (m, 1H), 7.90-7.96 (m, 1H), 7.75-7.78 (m, 2H), 7.63-7.67 (m, 2H), 7.52 (d, J=7.9 Hz, 1H), 4.83-4.86 (m, 4H), 3.87 (s, 3H), 3.16-3.22 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 382 (M+H)⁺.

Example 273 2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic acid

The title compound was prepared as described in Example 1B, substituting methyl 2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylate for methyl 4-(isoindoline-2-carboxamido)benzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 12.90-13.07 (bs, 1H), 8.62 (s, 1H), 8.26 (t, J=5.7 Hz, 1H), 7.88-7.93 (m, 2H), 7.75-7.78 (m, 2H), 7.63-7.67 (m, 2H), 7.49 (d, J=7.9 Hz, 1H), 4.83-4.85 (bs, 4H), 3.16-3.24 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); (ESI(+)) m/e 368 (M+H)⁺.

Example 274 5-amino-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

A solution of 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide (37 mg, 0.1 mmol) in 1 ml dimethylformamide in the presence of 11 mg of 10% Pd on carbon was treated with a hydrogen balloon overnight at room temperature. The suspension was filtered through diatomaceous earth and purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.51 (s, 1H), 8.24 (t, J=5.6 Hz, 1H), 7.74-7.78 (m, 2H), 7.62-7.66 (m, 2H), 7.19 (d, J=7.9 Hz, 1H), 6.78-6.89 (m, 2H), 4.67-4.71 (m, 4H), 3.15-3.26 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 339 (M+H)⁺.

Example 275 5-(hydroxymethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

A solution of calcium chloride (0.031 g, 0.277 mmol) in ethanol (0.8 mL) was added to a suspension of methyl 2-(4-(propylcarbamoyl)phenylcarbamoyl)isoindoline-5-carboxylate (0.04 g, 0.105 mmol) in tetrahydrofuran (1 mL). Sodium borohydride (0.02 g, 0.524 mmol) was then added in one portion and the suspension stirred at room temperature. After 18 hours, the mixture was concentrated to remove tetrahydrofuran then saturated aqueous sodium bicarbonate and water was added. The suspension was filtered and the solid was flash chromatographed to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (s, 1H), 8.25 (t, J=5.6 Hz, 1H), 7.74-7.78 (m, 2H), 7.64-7.67 (m, 2H), 7.31 (d, J=4.0 Hz, 1H), 7.30 (d, J=2.3 Hz, 1H), 7.26 (d, J=8.0 Hz, 1H), 5.19 (t, J=5.6 Hz, 1H), 4.71-4.78 (m, 4H), 4.52 (d, J=5.4 Hz, 2H), 3.15-3.25 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 354 (M+H)⁺.

Example 276 5-(aminomethyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

5-Cyano-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide (0.04 g, 0.115 mmol) and 7M ammonia-methanol/tetrahydrofuran/methanol (4 mL) were added to Ra—Ni 2800, water slurry (0.080 g, 1.363 mmol) in a 50 ml pressure bottle and stirred for 16 hours at 30 psi and room temperature. The mixture was filtered through a nylon membrane, concentrated and purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, Methanol-d₄) δ ppm 7.76-7.79 (m, 2H), 7.60-7.63 (m, 2H), 7.31-7.35 (m, 3H), 4.82 (s, 4H), 3.86 (s, 2H), 3.30-3.33 (m, 2H), 1.53-1.75 (m, 2H), 0.98 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 425 (M+H)⁺.

Example 277 5-[(2-hydroxy-2-methylpropanoyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 2-hydroxy-2-methylpropanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.59 (s, 1H), 8.55 (s, 1H), 8.25 (t, J=5.7 Hz, 1H), 7.81 (s, 1H), 7.74-7.78 (m, 2H), 7.62-7.68 (m, 2H), 7.59-7.64 (m, 1H), 7.28 (d, J=8.3 Hz, 1H), 5.71-5.75 (m, 1H), 4.72-4.80 (m, 4H), 3.16-3.23 (m, 2H), 1.42-1.59 (m, 2H), 1.36 (s, 6H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 425 (M+H)⁺.

Example 278 5-acetamido-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

A solution of 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide (0.035 g, 0.103 mmol) in dimethylformamide (0.7 mL) was treated with N,N-diisopropylethylamine (0.018 mL, 0.103 mmol) followed by acetyl chloride (0.011 g, 0.134 mmol) and the reaction solution was stirred at room temperature for 16 hours. The reaction was concentrated and purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.97 (s, 1H), 8.52 (s, 1H), 8.25 (t, J=5.7 Hz, 1H), 7.74-7.78 (m, 2H), 7.65-7.67 (m, 1H), 7.62-7.67 (m, 2H), 7.43 (dd, J=8.2, 1.9 Hz, 1H), 7.27 (d, J=8.2 Hz, 1H), 4.71-4.76 (m, 4H), 3.16-3.21 (m, 2H), 2.04 (s, 3H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 381 (M+H)⁺.

Example 279 5-[(N,N-dimethylglycyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 2-(dimethylamino)acetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.76 (s, 1H), 8.54 (s, 1H), 8.25 (t, J=5.6 Hz, 1H), 7.74-7.78 (m, 2H), 7.73 (d, J=1.8 Hz, 1H), 7.63-7.67 (m, 2H), 7.54 (dd, J=8.2, 1.9 Hz, 1H), 7.28 (d, J=8.2 Hz, 1H), 4.72-4.76 (m, 4H), 3.16-3.24 (m, 2H), 3.07 (s, 2H), 2.28 (s, 6H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(−)) m/e 422 (M−H)⁻.

Example 280 N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

In a 4 mL vial, a solution of 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide (50 mg, 0.12 mmol) and 1H-pyrazol-3-ylboronic acid (17 mg, 0.15 mmol) in dimethylformamide was treated with saturated aqueous sodium bicarbonate followed by bis(triphenylphosphine)palladium(II) chloride (7 mg). The vial was capped under nitrogen and the reaction heated at 85° C. for 6 hours. The reaction was cooled to ambient temperature and water was added. The resulting suspension was stirred for 5 minutes and filtered. The solid collected was washed with water and dried under vacuum; the solid was purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 12.39-13.18 (bs, 1H), 8.59 (s, 1H), 8.24-8.28 (m, 1H), 7.75-7.79 (m, 2H), 7.70-7.80 (m, 3H), 7.62-7.69 (m, 2H), 7.40 (d, J=7.9 Hz, 1H), 6.73 (d, J=2.2 Hz, 1H), 4.79-4.83 (m, 4H), 3.15-3.25 (m, 2H), 1.46-1.57 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 390 (M+H)⁺.

Example 281 N-[4-(propylcarbamoyl)phenyl]-5-(1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 10.91-13.69 (bs, 1H), 8.58 (s, 1H), 8.26 (t, J=5.7 Hz, 1H), 8.07-8.08 (bs, 2H), 7.75-7.79 (m, 2H), 7.67 (s, 1H), 7.54-7.65 (m, 2H), 7.57 (d, J=7.8 Hz, 1H), 7.34 (d, J=7.8 Hz, 1H), 4.76-4.79 (m, 4H), 3.15-3.25 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 390 (M+H)⁺.

Example 282 5-[(methoxyacetyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting 2-methoxyacetyl chloride for acetyl chloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.80 (s, 1H), 8.54 (s, 1H), 8.25 (t, J=5.7 Hz, 1H), 7.74-7.79 (m, 2H), 7.72-7.74 (m, 1H), 7.63-7.67 (m, 2H), 7.55 (dd, J=8.2, 1.9 Hz, 1H), 7.30 (d, J=8.2 Hz, 1H), 4.72-4.77 (m, 4H), 4.00 (s, 2H), 3.38 (s, 3H), 3.17-3.19 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 411 (M+H)⁺.

Example 283 5-[(methylsulfonyl)amino]-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

A solution of 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide (0.035 g, 0.103 mmol), pyridine (0.017 mL, 0.207 mmol) and catalytic N,N-dimethylaminopyridine in dimethylformamide (0.7 mL) was cooled to 0° C. Methanesulfonyl chloride (0.014 g, 0.126 mmol) was added and the reaction solution was allowed to stir at room temperature for 2 hours. The reaction mixture was concentrated and purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.74 (s, 1H), 8.54 (s, 1H), 8.26 (t, J=5.6 Hz, 1H), 7.74-7.78 (m, 2H), 7.63-7.66 (m, 2H), 7.32 (d, J=8.1 Hz, 1H), 7.14-7.20 (m, 2H), 4.73-4.76 (m, 4H), 3.15-3.25 (m, 2H), 2.98 (s, 3H), 1.45-1.62 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 417 (M+H)⁺.

TABLE 4 The following Examples were prepared essentially as described in Example 1, substituting 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine, 5,7-dihydro-6H-pyrrolo[3,4-b]pyridine, or 6,7-dihydro-5H-pyrrolo[3,4-d]pyrimidine for isoindoline in Example 1A and using an appropriate amine as described in Example 1C. Some products were purified by flash chromatography while others were purified by reverse-phase HPLC; some compounds also required Boc-deprotection after amide coupling as described in Example 2D. Accordingly, some Examples were isolated as trifluoroacetic acid salts. Ex Name ¹H NMR MS 285 N-{4-[(3,5- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.80 (t, J = 6.0 Hz, (ESI(+)) dimethoxybenzyl)carbamoyl]phenyl}- 1H), 8.66 (s, 1H), 8.61 (s, 1H), 8.50 (d, J = 5.0 Hz, m/e 433 1,3- 1H), 7.80-7.84 (m, 2H), 7.65-7.69 (m, 2H), 7.44 (d, J = 5.1 Hz, (M + H)⁺ dihydro-2H- 1H), 6.48 (d, J = 2.3 Hz, 2H), 6.37 (t, J = 2.3 Hz, pyrrolo[3,4-c]pyridine- 1H), 4.81-4.85 (m, 4H), 4.39 (d, J = 5.9 Hz, 2H), 2-carboxamide 3.31 (s, 6H) 286 N-{4-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.88 (t, J = 6.0 Hz, (ESI(+)) chlorobenzyl)carbamoyl]phenyl}- 1H), 8.66 (s, 1H), 8.61 (s, 1H), 8.50 (d, J = 5.0 Hz, m/e 407 1,3- 1H), 7.80-7.84 (m, 2H), 7.65-7.69 (m, 2H), (M + H)⁺ dihydro-2H- 7.32-7.45 (m, 5H), 4.78-4.88 (m, 4H), 4.44 (d, J = 5.9 Hz, 2H) pyrrolo[3,4-c]pyridine- 2-carboxamide 287 N-(4-{[4-(pyridin-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61-8.64 (m, (ESI(+)) yl)piperazin-1- 2H), 8.51 (d, J = 5.0 Hz, 1H), 8.13 (ddd, J = 4.9, 2.0, m/e 429 yl]carbonyl}phenyl)- 0.8 Hz, 1H), 7.64-7.68 (m, 2H), 7.56 (ddd, J = 8.7, (M + H)⁺ 1,3-dihydro-2H- 7.0, 1.9 Hz, 1H), 7.44 (d, J = 5.1 Hz, 1H), pyrrolo[3,4-c]pyridine- 7.36-7.40 (m, 2H), 6.85 (d, J = 8.6 Hz, 1H), 6.65-6.69 (m, 1H), 2-carboxamide 4.81-4.85 (m, 4H), 3.53-3.63 (m, 8H) 288 N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61-8.64 (m, (ESI(+)) phenylpropyl)carbamoyl]phenyl}- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.27-8.31 (m, 1H), m/e 401 1,3- 7.75-7.79 (m, 2H), 7.63-7.67 (m, 2H), 7.44 (d, J = 5.1 Hz, (M + H)⁺ dihydro-2H- 1H), 7.15-7.31 (m, 5H), 4.76-4.89 (m, 4H), pyrrolo[3,4-c]pyridine- 3.20-3.32 (m, 2H), 2.63 (t, J = 7.6 Hz, 2H), 1.77-1.88 (m, 2H) 2-carboxamide 289 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (s, 1H), (ESI(+)) [(tetrahydrofuran-3- 8.61 (s, 1H), 8.50 (d, J = 5.0 Hz, 1H), 8.39 (t, J = 5.7 Hz, m/e 367 ylmethyl)carbamoyl]phenyl}- 1H), 7.75-7.79 (m, 2H), 7.63-7.68 (m, 2H), (M + H)⁺ 1,3-dihydro- 7.44 (d, J = 5.1 Hz, 1H), 4.81-4.84 (m, 4H), 3.57-3.78 (m, 2H-pyrrolo[3,4- 3H), 3.48 (dd, J = 8.5, 5.3 Hz, 1H), 3.14-3.30 (m, 2H), c]pyridine-2- 2.41-2.51 (m, 1H), 1.87-2.12 (m, 1H), 1.54-1.66 (m, carboxamide 1H) 290 N-{4-[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61-8.64 (m, (ESI(+)) methylbutyl)carbamoyl]phenyl}- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.21 (t, J = 5.6 Hz, 1H), m/e 353 1,3-dihydro- 7.74-7.78 (m, 2H), 7.62-7.66 (m, 2H), 7.44 (d, J = 5.1 Hz, (M + H)⁺ 2H-pyrrolo[3,4- 1H), 4.81-4.84 (m, 4H), 3.20-3.33 (m, 2H), c]pyridine-2- 1.53-1.69 (m, 1H), 1.37-1.45 (m, 2H), 0.91 (d, J = 6.6 Hz, carboxamide 6H) 426 N-(4-{[(2S)- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (s, 1H), (ESI(−)) tetrahydrofuran-2- 8.61 (s, 1H), 8.50 (d, J = 5.0 Hz, 1H), 8.33 (t, J = 5.8 Hz, m/e 367 ylmethyl]carbamoyl}phenyl)- 1H), 7.76-7.81 (m, 2H), 7.63-7.67 (m, 2H), (M + H)⁻ 1,3-dihydro- 7.44 (d, J = 5.1 Hz, 1H), 4.76-4.89 (m, 4H), 3.96 (p, J = 6.3 Hz, 2H-pyrrolo[3,4- 1H), 3.73-3.82 (m, 1H), 3.58-3.67 (m, 1H), c]pyridine-2- 3.26-3.35 (m, 2H), 1.73-1.98 (m, 3H), 1.52-1.66 (m, 1H) carboxamide 427 N-(4-{[(2R)- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.63-8.65 (bs, (ESI(−)) tetrahydrofuran-2- 1H), 8.61-8.62 (bs, 1H), 8.50 (d, J = 5.0 Hz, 1H), m/e 411 ylmethyl]carbamoyl}phenyl)- 8.32 (t, J = 5.8 Hz, 1H), 7.76-7.81 (m, 2H), 7.63-7.67 (m, (M − H)⁺ 1,3-dihydro- 2H), 7.44 (d, J = 5.1 Hz, 1H), 4.81-4.88 (m, 4H), 2H-pyrrolo[3,4- 3.97 (p, J = 6.2 Hz, 1H), 3.74-3.82 (m, 1H), 3.58-3.66 (m, c]pyridine-2- 1H), 3.26-3.32 (m, 2H), 1.74-1.96 (m, 3H), carboxamide 1.53-1.64 (m, 1H) 430 N-(4-{[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.10-9.12 (bs, (APCI(+)) methylbutyl)amino]carbonyl}phenyl)- 1H), 8.83 (s, 1H), 8.67 (s, 1H), 8.22 (t, J = 5.6 Hz, m/e 354 5,7- 1H), 7.75-7.79 (m, 2H), 7.63-7.67 (m, 2H), (M + H)⁺ dihydro-6H- 4.81-4.84 (m, 4H), 3.20-3.34 (m, 2H), 1.53-1.69 (m, 1H), pyrrolo[3,4- 1.37-1.45 (m, 2H), 0.91 (d, J = 6.6 Hz, 6H) d]pyrimidine-6- carboxamide 431 N-(4-{[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.11 (s, 1H), (APCI(+)) phenylpropyl)amino]carbonyl}phenyl)- 8.83 (s, 1H), 8.68 (s, 1H), 8.30 (t, J = 5.6 Hz, 1H), m/e 402 5,7- 7.76-7.80 (m, 2H), 7.64-7.68 (m, 2H), 7.15-7.32 (m, (M + H)⁺ dihydro-6H- 5H), 4.77-4.89 (m, 4H), 3.21-3.34 (m, 2H), pyrrolo[3,4- 2.60-2.74 (m, 2H), 2.29-1.90 (m, 2H) d]pyrimidine-6- carboxamide 437 N-[4-({[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.66 (s, 1H), (ESI(+)) hydroxy-1- 8.61 (s, 1H), 8.51 (d, J = 2.0 Hz, 1H), 8.49 (d, J = 5.2 Hz, m/e 403 phenylethyl]amino}carbonyl)phenyl]- 1H), 7.82-7.87 (m, 2H), 7.66-7.70 (m, 2H), (M + H)⁺ 1,3- 7.38-7.45 (m, 3H), 7.29-7.34 (m, 2H), 7.19-7.26 (m, 1H), dihydro-2H- 5.03-5.10 (m, 1H), 4.90 (t, J = 5.8 Hz, 1H), pyrrolo[3,4-c]pyridine- 4.79-4.87 (m, 4H), 3.61-3.76 (m, 2H) 2-carboxamide 445 N-[4-({[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.68 (s, 1H), (ESI(+)) hydroxy-1-pyridin-2- 8.62 (s, 1H), 8.44-8.54 (m, 3H), 7.84-7.89 (m, 2H), m/e 404 ylethyl]amino}carbonyl)phenyl]- 7.75 (td, J = 7.7, 1.8 Hz, 1H), 7.66-7.72 (m, 2H), (M + H)⁺ 1,3-dihydro- 7.39-7.45 (m, 2H), 7.26 (ddd, J = 7.5, 4.8, 1.2 Hz, 1H), 2H-pyrrolo[3,4- 5.10-5.17 (m, 1H), 4.90 (t, J = 6.0 Hz, 1H), c]pyridine-2- 4.79-4.87 (m, 4H), 3.73-3.88 (m, 2H) carboxamide 446 N-(4-{[(3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.62 (s, 1H), (ESI(+)) methylbutyl)amino]carbonyl}phenyl)- 8.48 (dd, J = 4.9, 1.5 Hz, 1H), 8.22 (t, J = 5.6 Hz, 1H), m/e 353 5,7- 7.81 (dd, J = 7.7, 1.5 Hz, 1H), 7.73-7.79 (m, 2H), (M + H)⁺ dihydro-6H- 7.64-7.68 (m, 2H), 7.33 (dd, J = 7.7, 4.9 Hz, 1H), pyrrolo[3,4-b]pyridine- 4.78-4.80 (bs, 4H), 3.21-3.33 (m, 2H), 1.61 (dp, J = 13.3, 6-carboxamide 6.6 Hz, 1H), 1.41 (q, J = 7.1 Hz, 2H), 0.90 (d, J = 6.6 Hz, 6H) 447 N-(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.63 (s, 1H), (ESI(+)) {[(tetrahydrofuran-3- 8.48 (dd, J = 4.9, 1.5 Hz, 1H), 8.39 (t, J = 5.7 Hz, 1H), m/e 367 ylmethyl)amino]carbonyl}phenyl)- 7.76-7.83 (m, 3H), 7.65-7.69 (m, 2H), 7.33 (dd, J = 7.7, (M + H)⁺ 5,7- 4.9 Hz, 1H), 4.78-4.81 (bs, 4H), 3.57-3.82 (m, dihydro-6H- 3H), 3.44-3.51 (m, 1H), 3.17-3.28 (m, 2H), pyrrolo[3,4-b]pyridine- 2.42-2.50 (m, 1H), 1.85-2.02 (m, 1H), 1.54-1.68 (m, 1H) 6-carboxamide 448 N-{4-[(4-pyridin-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), (ESI(+)) ylpiperazin-1- 8.49 (dd, J = 4.9, 1.5 Hz, 1H), 8.13 (dd, J = 5.0, 1.9 Hz, m/e 429 yl)carbonyl]phenyl}- 1H), 7.81 (dd, J = 7.7, 1.5 Hz, 1H), 7.66-7.70 (m, (M + H)⁺ 5,7-dihydro-6H- 2H), 7.56 (ddd, J = 8.7, 7.0, 1.8 Hz, 1H), pyrrolo[3,4-b]pyridine- 7.36-7.41 (m, 2H), 7.34 (dd, J = 7.7, 5.0 Hz, 1H), 6.85 (d, J = 8.6 Hz, 6-carboxamide 1H), 6.67 (dd, J = 6.9, 4.8 Hz, 1H), 4.79-4.81 (bs, 4H), 3.43-3.75 (m, 8H) 553 N-{4-[(tetrahydro-2H- ¹H NMR (300 MHz, DMSO-d₆) δ 8.64 (s, 1H), (ESI(+)) pyran-2- 8.61 (s, 1H), 8.50 (d, J = 5.0 Hz, 1H), 8.29 (t, J = 5.8 Hz, m/e 381 ylmethyl)carbamoyl]phenyl}- 1H), 7.82-7.75 (m, 2H), 7.68-7.61 (m, 2H), 7.44 (d, (M + H)⁺ 1,3-dihydro- J = 5.1 Hz, 1H), 4.86-4.79 (m, 4H), 3.87 (dd, J = 11.3, 2H-pyrrolo[3,4- 3.0 Hz, 1H), 3.48-3.34 (m, 2H), 3.28-3.17 (m, c]pyridine-2- 2H), 1.82-1.72 (m, 1H), 1.66-1.56 (m, 1H), carboxamide 1.56-1.33 (m, 3H), 1.28-1.07 (m, 1H) 554 N-{4-[(tetrahydro-2H- ¹H NMR (300 MHz, DMSO-d₆) δ 8.63 (d, J = 8.3 Hz, (ESI(+)) pyran-3- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.28 (t, J = 5.7 Hz, 1H), m/e 381 ylmethyl)carbamoyl]phenyl}- 7.77 (d, J = 8.8 Hz, 2H), 7.65 (d, J = 8.8 Hz, 2H), (M + H)⁺ 1,3-dihydro- 7.44 (d, J = 5.0 Hz, 1H), 4.83 (d, J = 4.3 Hz, 4H), 2H-pyrrolo[3,4- 3.82-3.64 (m, 2H), 3.18-3.04 (m, 3H), 1.78 (dd, J = 6.9, c]pyridine-2- 3.6 Hz, 2H), 1.58 (dd, J = 10.2, 6.6 Hz, 1H), carboxamide 1.53-1.36 (m, 1H), 1.31-1.17 (m, 1H) 555 N-{4-[(tetrahydro-2H- ¹H NMR (300 MHz, DMSO-d₆) δ 8.66-8.59 (m, 2H), (ESI(+)) pyran-4- 8.50 (d, J = 5.0 Hz, 1H), 8.33-8.25 (m, 1H), m/e 381 ylmethyl)carbamoyl]phenyl}- 7.81-7.74 (m, 2H), 7.69-7.61 (m, 2H), 7.44 (d, J = 5.0 Hz, (M + H)⁺ 1,3-dihydro- 1H), 4.82 (bs, 4H), 3.89-3.79 (m, 2H), 3.24 (d, J = 11.6 Hz, 2H-pyrrolo[3,4- 1H), 3.14 (t, J = 6.1 Hz, 2H), 1.86-1.69 (m, c]pyridine-2- 1H), 1.64-1.54 (m, 2H), 1.27-1.06 (m, 3H) carboxamide 556 N-(4-{[(2S)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.66-8.59 (m, 2H), (ESI(+)) hydroxy-4- 8.50 (d, J = 5.0 Hz, 1H), 7.83-7.75 (m, 3H), m/e 383 methylpentan-2- 7.69-7.61 (m, 2H), 7.44 (d, J = 5.1 Hz, 1H), 4.91-4.80 (m, (M + H)⁺ yl]carbamoyl}phenyl)- 4H), 4.64 (t, J = 5.7 Hz, 1H), 4.12-3.99 (m, 1H), 1,3-dihydro-2H- 3.41 (d, J = 5.3 Hz, 1H), 1.69-1.54 (m, 1H), pyrrolo[3,4-c]pyridine- 1.53-1.31 (m, 2H), 0.88 (t, J = 6.7 Hz, 6H) 2-carboxamide 599 N-[4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.62 (d, J = 4.9 Hz, (ESI(+)) (propylcarbamoyl)phenyl]- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.30-8.20 (m, 1H), m/e 325 1,3-dihydro-2H- 7.83-7.72 (m, 2H), 7.68-7.59 (m, 2H), 7.44 (d, J = 5.1 Hz, (M + H)⁺ pyrrolo[3,4-c]pyridine- 1H), 4.87-4.77 (m, 4H), 3.22-3.13 (m, 2H), 2-carboxamide 1.61-1.45 (m, 2H), 0.89 (t, J = 7.4 Hz, 3H) 600 N-(4-{[(2S)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.63 (s, 1H), (ESI(+)) tetrahydrofuran-2- 8.48 (dd, J = 4.9, 1.5 Hz, 1H), 8.34 (t, J = 5.8 Hz, 1H), m/e 367 ylmethyl]carbamoyl}phenyl)- 7.85-7.75 (m, 3H), 7.70-7.63 (m, 2H), 7.33 (dd, J = 7.7, (M + H)⁺ 5,7-dihydro- 4.9 Hz, 1H), 4.80 (bs, 4H), 3.97 (p, J = 6.2 Hz, 1H), 6H-pyrrolo[3,4- 3.83-3.72 (m, 1H), 3.68-3.57 (m, 1H), 3.28 (dd, J = 5.9, b]pyridine-6- 1.7 Hz, 1H), 1.98-1.72 (m, 3H), 1.66-1.51 (m, carboxamide 1H) 601 N-(4-{[(2R)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (s, 1H), (ESI(+)) tetrahydrofuran-2- 8.48 (dd, J = 4.9, 1.5 Hz, 1H), 8.32 (t, J = 5.8 Hz, 1H), m/e 367 ylmethyl]carbamoyl}phenyl)- 7.85-7.75 (m, 3H), 7.70-7.63 (m, 2H), 7.33 (dd, J = 7.7, (M + H)⁺ 5,7-dihydro- 4.9 Hz, 1H), 4.80 (bs, 4H), 3.97 (p, J = 6.2 Hz, 1H), 6H-pyrrolo[3,4- 3.83-3.72 (m, 1H), 3.68-3.57 (m, 1H), b]pyridine-6- 1.98-1.72 (m, 3H), 1.69-1.51 (m, 1H) carboxamide 602 N-(4-{[(2S)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), (ESI(+)) hydroxy-4- 8.48 (dd, J = 4.9, 1.5 Hz, 1H), 7.87-7.71 (m, 4H), m/e 383 methylpentan-2- 7.70-7.63 (m, 2H), 7.33 (dd, J = 7.7, 4.9 Hz, 1H), 4.79 (bs, (M + H)⁺ yl]carbamoyl}phenyl)- 4H), 4.13-3.95 (m, 1H), 3.42 (dd, J = 10.6, 5.4 Hz, 5,7-dihydro-6H- 2H), 1.72-1.54 (m, 1H), 1.53-1.31 (m, 2H), 0.88 (t, pyrrolo[3,4-b]pyridine- J = 6.7 Hz, 6H) 6-carboxamide 603 N-(4-{[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.64 (s, 1H), (ESI(+)) hydroxy-1- 8.53-8.45 (m, 2H), 7.88-7.78 (m, 3H), 7.73-7.66 (m, m/e 403 phenylethyl]carbamoyl}phenyl)- 2H), 7.47-7.27 (m, 5H), 7.27-7.18 (m, 1H), (M + H)⁺ 5,7-dihydro- 5.12-5.01 (m, 1H), 4.90 (t, J = 5.8 Hz, 1H), 4.80 (bs, 4H), 6H-pyrrolo[3,4- 3.78-3.59 (m, 2H) b]pyridine-6- carboxamide 604 N-{4-[(tetrahydro-2H- ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (s, 1H), (ESI(+)) pyran-4- 8.48 (dd, J = 4.9, 1.5 Hz, 1H), 8.30 (t, J = 5.8 Hz, 1H), m/e 381 ylmethyl)carbamoyl]phenyl}- 7.85-7.74 (m, 3H), 7.70-7.63 (m, 2H), 7.33 (dd, J = 7.7, (M + H)⁺ 5,7-dihydro- 4.9 Hz, 1H), 4.79 (bs, 4H), 3.89-3.79 (m, 2H), 6H-pyrrolo[3,4- 3.28-3.19 (m, 2H), 3.14 (t, J = 6.3 Hz, 2H), 1.87-1.70 (m, b]pyridine-6- 1H), 1.64-1.54 (m, 2H), 1.29-1.01 (m, 2H) carboxamide 613 N-(4-{[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.65 (s, 1H), (ESI(+)) hydroxy-1-(pyridin-2- 8.55-8.51 (m, 1H), 8.47 (t, J = 6.7 Hz, 2H), 7.87 (d, J = 8.8 Hz, m/e 404 yl)ethyl]carbamoyl}phenyl)- 2H), 7.84-7.79 (m, 1H), 7.76 (dd, J = 7.7, 1.8 Hz, (M + H)⁺ 5,7-dihydro-6H- 1H), 7.71 (t, J = 5.4 Hz, 2H), 7.41 (d, J = 7.8 Hz, pyrrolo[3,4-b]pyridine- 1H), 7.33 (dd, J = 7.7, 4.9 Hz, 1H), 7.29-7.22 (m, 6-carboxamide 1H), 5.19-5.09 (m, 1H), 4.90 (t, J = 5.9 Hz, 1H), 4.80 (bs, 4H), 3.90-3.72 (m, 2H) 627 N-{4-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (d, J = 5.9 Hz, (ESI(+)) hydroxypiperidin-1- 2H), 8.50 (d, J = 5.0 Hz, 1H), 7.62 (d, 2H), 7.44 (d, J = 5.1 Hz, m/e 367 yl)carbonyl]phenyl}- 1H), 7.30 (d, 2H), 4.82 (d, J = 4.3 Hz, 4H), (M + H)⁺ 1,3-dihydro-2H- 4.76 (d, J = 4.0 Hz, 1H), 3.73 (td, J = 8.3, 4.2 Hz, 2H), pyrrolo[3,4-c]pyridine- 3.22-3.08 (m, 2H), 1.82-1.65 (m, 2H), 2-carboxamide 1.43-1.26 (m, 2H) 628 N-{4-[(2-hydroxy-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.64 (d, J = 12.5 Hz, (ESI(+)) methylpropyl)carbamoyl]phenyl}- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.06 (t, J = 6.0 Hz, m/e 355 1,3- 1H), 7.80 (d, J = 8.8 Hz, 2H), 7.66 (d, J = 8.8 Hz, 2H), (M + H)⁺ dihydro-2H- 7.44 (d, J = 5.1 Hz, 1H), 4.83 (d, J = 4.3 Hz, 4H), pyrrolo[3,4-c]pyridine- 4.56 (s, 1H), 3.24 (d, J = 6.0 Hz, 2H), 2.89 (s, 1H), 1.10 (s, 2-carboxamide 6H) 629 N-{4-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (d, J = 6.4 Hz, (ESI(+)) hydroxybutyl)carbamoyl]phenyl}- 1H), 8.50 (d, J = 5.0 Hz, 1H), 8.26 (t, J = 5.6 Hz, 1H), m/e 355 1,3- 7.76 (d, J = 8.8 Hz, 1H), 7.64 (d, J = 8.8 Hz, 1H), (M + H)⁺ dihydro-2H- 7.44 (d, J = 5.1 Hz, 1H), 4.82 (d, J = 4.3 Hz, 1H), 4.39 (t, J = 5.1 Hz, pyrrolo[3,4-c]pyridine- 1H), 3.41 (q, J = 6.1 Hz, 1H), 2-carboxamide 3.25-3.15 (m, 2H), 1.59-1.38 (m, 4H) 630 N-(4-{[(2S)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (d, J = 6.0 Hz, (ESI(+)) hydroxy-3- 2H), 8.50 (d, J = 5.0 Hz, 1H), 7.83-7.77 (m, 2H), m/e 369 methylbutan-2- 7.74 (d, J = 8.9 Hz, 1H), 7.64 (d, J = 1.8 Hz, 1H), (M + H)⁺ yl]carbamoyl}phenyl)- 7.44 (d, J = 5.1 Hz, 1H), 4.83 (d, J = 4.3 Hz, 4H), 4.53 (t, J = 5.6 Hz, 1,3-dihydro-2H- 1H), 3.90-3.70 (m, 1H), 3.51 (t, J = 5.8 Hz, pyrrolo[3,4-c]pyridine- 2H), 1.92 (dq, J = 13.6, 6.8 Hz, 1H), 0.89 (dd, J = 7.9, 2-carboxamide 6.9 Hz, 6H) 631 N-{4-[(1-hydroxy-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (d, J = 4.0 Hz, (ESI(+)) methylpropan-2- 1H), 8.50 (d, J = 5.0 Hz, 1H), 7.73 (d, J = 8.9 Hz, 1H), m/e 355 yl)carbamoyl]phenyl}- 7.64 (d, J = 8.9 Hz, 1H), 7.44 (d, J = 5.1 Hz, 1H), (M + H)⁺ 1,3-dihydro-2H- 7.35 (s, 1H), 4.94 (t, J = 5.9 Hz, 1H), 4.82 (d, J = 4.3 Hz, pyrrolo[3,4-c]pyridine- 1H), 3.49 (d, J = 6.0 Hz, 2H), 1.31 (s, 6H) 2-carboxamide 632 N-(4-{[(2R)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.63 (d, J = 9.3 Hz, (ESI(+)) hydroxypropyl]carbamoyl}phenyl)- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.21 (t, J = 5.7 Hz, 1H), m/e 341 1,3- 7.79 (d, J = 8.8 Hz, 2H), 7.65 (d, J = 8.8 Hz, 2H), (M + H)⁺ dihydro-2H- 7.44 (d, J = 5.0 Hz, 1H), 4.83 (d, J = 4.2 Hz, 4H), 4.72 (d, J = 4.7 Hz, pyrrolo[3,4-c]pyridine- 1H), 3.77 (dt, J = 11.9, 6.1 Hz, 1H), 2-carboxamide 3.24-3.09 (m, 2H), 3.05 (s, 1H), 1.06 (d, J = 6.2 Hz, 3H) 633 N-(4-{[(2S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.63 (d, J = 8.5 Hz, (ESI(+)) hydroxypropyl]carbamoyl}phenyl)- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.20 (t, J = 5.7 Hz, 1H), m/e 341 1,3- 7.79 (d, J = 8.8 Hz, 1H), 7.65 (d, J = 8.8 Hz, 1H), (M + H)⁺ dihydro-2H- 7.44 (d, J = 5.1 Hz, 1H), 4.83 (d, J = 4.3 Hz, 4H), 4.72 (d, J = 4.7 Hz, pyrrolo[3,4-c]pyridine- 1H), 3.87-3.68 (m, 1H), 3.17 (ddd, J = 15.1, 2-carboxamide 9.4, 3.6 Hz, 2H), 1.06 (d, J = 6.3 Hz, 3H) 634 N-(4-{[3-(piperidin-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.63 (d, J = 11.4 Hz, (ESI(+)) yl)propyl]carbamoyl}phenyl)- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.35 (t, J = 5.4 Hz, m/e 408 1,3-dihydro- 1H), 7.76 (d, J = 8.8 Hz, 2H), 7.65 (d, J = 8.8 Hz, 2H), (M + H)⁺ 2H-pyrrolo[3,4- 7.44 (d, J = 5.0 Hz, 1H), 4.82 (d, J = 4.3 Hz, 4H), c]pyridine-2- 2.37-2.22 (m, 6H), 1.72-1.59 (m, 10H), 1.54-1.43 (m, carboxamide 20H), 1.38 (d, J = 4.8 Hz, 10H) 635 N-[4-(5,6- ¹H NMR (300 MHz, DMSO-d₆) δ 8.64 (d, J = 11.8 Hz, (ESI(+)) dihydroimidazo[1,5- 2H), 8.51 (d, J = 5.0 Hz, 1H), 7.68 (d, J = 8.6 Hz, m/e 389 a]pyrazin-7(8H)- 2H), 7.61 (s, 1H), 7.43 (t, J = 6.9 Hz, 3H), 4.83 (d, J = 4.3 Hz, (M + H)⁺ ylcarbonyl)phenyl]- 4H), 4.74 (s, 2H), 4.12 (t, J = 5.4 Hz, 2H), 1,3-dihydro-2H- 3.84 (s, 2H) pyrrolo[3,4-c]pyridine- 2-carboxamide 686 N-[4-(morpholin-4- ¹H NMR (500 MHz, DMSO-d₆, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)phenyl]- 8.69 (s, 1H), 8.55 (d, J = 3.7, 2H), 7.72 (d, J = 5.6, 1H), m/e 353 1,3-dihydro-2H- 7.48-7.39 (m, 2H), 7.21-7.11 (m, 2H), 4.76 (d, J = 23.4, (M + H)⁺ pyrrolo[3,4-c]pyridine- 4H), 3.40 (s, 8H) 2-carboxamide 687 N-(4-{[3-(2- ¹H NMR (500 MHz, DMSO-d₆, Temp = 90° C.) δ (ESI(+)) oxopyrrolidin-1- 8.88 (s, 1H), 8.76 (d, J = 5.7, 2H), 8.29 (t, J = 5.7, 1H), m/e 408 yl)propyl]carbamoyl}phenyl)- 7.91 (d, J = 5.7, 1H), 7.78 (m, 2H), 7.65 (m, 2H), (M + H)⁺ 1,3-dihydro- 4.98 (bs, 2H), 4.94 (bs, 2H), 3.35 (t, J = 7.0, 2H), 3.22 (m, 2H-pyrrolo[3,4- 4H), 2.22 (t, J = 8.0, 2H), 1.92 (m, 2H), 1.70 (p, J = 7.0, c]pyridine-2- 2H) carboxamide 723 N-{4-[(2- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1H) (ESI(+)) isopropoxyethyl)carbamoyl]phenyl}- 8.78 (d, J = 6.10 Hz, 1H) 8.02 (d, J = 5.80 Hz, 1H) m/e 369 1,3- 7.76-7.81 (m, 2H) 7.62-7.66 (m, 2H) 5.01 (d, J = 30.82 Hz, (M + H)⁺ dihydro-2H- 4H) 3.54-3.63 (m, 1H) 3.49 (t, J = 6.10 Hz, 2H) pyrrolo[3,4-c]pyridine- 3.38 (t, J = 6.10 Hz, 2H) 1.09 (d, J = 6.10 Hz, 6H) 2-carboxamide 724 N-{4-[methyl(3- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1 (ESI(+)) methylbutyl)carbamoyl]phenyl}- H) 8.79 (d, J = 6.10 Hz, 1H) 8.04 (d, J = 5.80 Hz, 1H) m/e 367 1,3-dihydro- 7.60 (d, J = 8.54 Hz, 2H) 7.32 (d, J = 7.63 Hz, 2H) (M + H)⁺ 2H-pyrrolo[3,4- 4.95-5.07 (m, 4H) 3.44 (s, 2H) 2.89-2.96 (m, 3H) c]pyridine-2- 1.44 (s, 3H) 0.83 (d, J = 107.41 Hz, 6H) carboxamide 725 N-[4-(azetidin-1- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.84 (s, 1H) (ESI(+)) ylcarbonyl)phenyl]- 8.74 (d, J = 5.80 Hz, 1H) 7.94 (d, J = 5.80 Hz, 1H) m/e 323 1,3-dihydro-2H- 7.60-7.64 (m, 2H) 7.56-7.59 (m, 2H) 4.98 (d, J = 24.72 Hz, (M + H)⁺ pyrrolo[3,4-c]pyridine- 4H) 4.34 (s, 2H) 4.05 (d, J = 6.71 Hz, 2H) 2-carboxamide 2.22-2.33 (m, 2H) 726 N-[4-(2,6- diazaspiro[3.5]non-2- ylcarbonyl)phenyl]- 1,3-dihydro-2H- pyrrolo[3,4-c]pyridine- 2-carboxamide 727 N-[4-(1,7- diazaspiro[4.4]non-1- ylcarbonyl)phenyl]- 1,3-dihydro-2H- pyrrolo[3,4-c]pyridine- 2-carboxamide 728 N-(4-{[4-(morpholin- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.90 (s, 1H) (ESI(+)) 4- 8.80 (d, J = 5.80 Hz, 1H) 8.05 (d, J = 5.80 Hz, 1H) m/e 458 yl)benzyl]carbamoyl}phenyl)- 7.80-7.85 (m, 2H) 7.61-7.68 (m, 2H) 7.27 (d, J = 8.54 Hz, (M + H)⁺ 1,3-dihydro- 2H) 7.05 (d, J = 8.85 Hz, 2H) 5.02 (d, J = 33.26 Hz, 2H-pyrrolo[3,4- 4H) 4.40 (s, 2H) 3.76-3.81 (m, 4H) c]pyridine-2- 3.16-3.19 (m, 4H) carboxamide 729 N-{4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.90 (s, 1H) (ESI(+)) [(cyclopropylmethyl)carbamoyl]phenyl}- 8.79 (d, J = 5.80 Hz, 1H) 8.04 (d, J = 6.10 Hz, 1H) m/e 337 1,3- 7.78-7.82 (m, 2H) 7.62-7.67 (m, 2H) 5.02 (d, J = 31.73 Hz, (M + H)⁺ dihydro-2H- 4H) 3.14 (d, J = 7.02 Hz, 2H) 0.99-1.08 (m, 1H) pyrrolo[3,4-c]pyridine- 0.40-0.48 (m, 2H) 0.21-0.26 (m, 2H) 2-carboxamide 730 N-{4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1 (ESI(+)) [methyl(propyl)carbamoyl]phenyl}- H) 8.79 (d, J = 6.10 Hz, 1H) 8.04 (d, J = 5.80 Hz, 1H) m/e 339 1,3- 7.57-7.64 (m, 2H) 7.25-7.38 (m, 2H) 5.01 (d, (M + H)⁺ dihydro-2H- J = 32.04 Hz, 4H) 3.17-3.45 (m, 2H) 2.93 (s, 3H) pyrrolo[3,4-c]pyridine- 1.53 (d, J = 7.32 Hz, 2H) 0.64-0.97 (m, 3H) 2-carboxamide 731 N-[4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.90 (s, 1H) (ESI(+)) (isobutylcarbamoyl)phenyl]- 8.79 (d, J = 5.80 Hz, 1H) 8.04 (d, J = 5.80 Hz, 1H) m/e 339 1,3-dihydro-2H- 7.77-7.81 (m, 2H) 7.60-7.65 (m, 2H) 5.02 (d, J = 31.73 Hz, (M + H)⁺ pyrrolo[3,4-c]pyridine- 4H) 3.08 (d, J = 7.02 Hz, 2H) 1.79-1.89 (m, 1H) 2-carboxamide 0.89 (d, J = 6.71 Hz, 6H) 732 N-[4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.84 (s, 1H) (ESI(+)) (butylcarbamoyl)phenyl]- 8.74 (d, J = 5.80 Hz, 1H) 7.94 (d, J = 5.80 Hz, 1H) m/e 339 1,3-dihydro-2H- 7.76-7.79 (m, 2H) 7.61-7.65 (m, 2H) 4.98 (d, J = 24.41 Hz, (M + H)⁺ pyrrolo[3,4-c]pyridine- 4H) 3.25 (t, J = 7.02 Hz, 2H) 1.46-1.55 (m, 2H) 2-carboxamide 1.28-1.38 (m, 2H) 0.90 (t, J = 7.32 Hz, 3H) 733 N-{4-[(2- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.88 (s, 1H) (ESI(+)) methoxyethyl)carbamoyl]phenyl}- 8.78 (d, J = 5.80 Hz, 1H) 8.02 (d, J = 5.80 Hz, 1H) m/e 341 1,3- 7.77-7.81 (m, 2H) 7.60-7.65 (m, 2H) 5.01 (d, J = 29.90 Hz, (M + H)⁺ dihydro-2H- 4H) 3.40-3.50 (m, 4H) 3.27 (s, 3H) pyrrolo[3,4-c]pyridine- 2-carboxamide 734 N-[4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1 (ESI(+)) (cyclopentylcarbamoyl)phenyl]- H) 8.79 (d, J = 5.80 Hz, 1H) 8.03 (d, J = 6.10 Hz, 1H) m/e 351 1,3-dihydro- 7.77-7.81 (m, 2H) 7.60-7.65 (m, 2H) 5.01 (d, (M + H)⁺ 2H-pyrrolo[3,4- J = 31.43 Hz, 4H) 4.14-4.25 (m, 1H) 1.82-1.99 (m, c]pyridine-2- 2H) 1.64-1.78 (m, 2H) 1.47-1.58 (m, 4H) carboxamide 735 N-{4-[(3R)- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.90 (s, 1H) (ESI(+)) tetrahydrofuran-3- 8.80 (d, J = 6.10 Hz, 1H) 8.05 (d, J = 6.10 Hz, 1H) m/e 353 ylcarbamoyl]phenyl}- 7.79-7.83 (m, 2H) 7.61-7.67 (m, 2H) 5.02 (d, J = 32.65 Hz, (M + H)⁺ 1,3-dihydro-2H- 4H) 4.39-4.50 (m, 1H) 3.85-3.90 (m, 2H) pyrrolo[3,4-c]pyridine- 3.70-3.76 (m, 1H) 3.58 (dd, J = 8.85, 4.27 Hz, 1H) 2-carboxamide 2.11-2.23 (m, 1H) 1.89-1.97 (m, 1H) 736 N-{4-[(2- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.90 (s, 1H) (ESI(+)) methoxyethyl)(methyl)carbamoyl]phenyl}- 8.79 (d, J = 6.10 Hz, 1H) 8.04 (d, J = 5.80 Hz, 1H) m/e 355 1,3-dihydro-2H- 7.60 (d, J = 8.54 Hz, 2H) 7.34 (d, J = 8.54 Hz, 2H) 5.01 (d, (M + H)⁺ pyrrolo[3,4-c]pyridine- J = 31.73 Hz, 4H) 3.51 (d, J = 66.52 Hz, 4H) 2-carboxamide 3.15-3.34 (m, 3H) 2.94-3.02 (m, 3H) 737 N-{4-[(1- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1H) (ESI(+)) methoxypropan-2- 8.79 (d, J = 5.49 Hz, 1H) 8.03 (d, J = 6.10 Hz, 1H) m/e 355 yl)carbamoyl]phenyl}- 7.77-7.81 (m, 2H) 7.61-7.65 (m, 2H) 5.02 (d, J = 31.12 Hz, (M + H)⁺ 1,3-dihydro-2H- 4 H) 4.15-4.23 (m, 1H) 3.42 (dd, J = 9.61, 6.56 Hz, pyrrolo[3,4-c]pyridine- 1H) 3.30 (dd, J = 9.61, 5.95 Hz, 1H) 3.27 (s, 3H) 2-carboxamide 1.14 (d, J = 6.71 Hz, 3H) 738 N-{4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.88 (s, 1H) (ESI(+)) [(cyclopentylmethyl)carbamoyl]phenyl}- 8.78 (d, J = 5.80 Hz, 1H) 8.01 (d, J = 5.80 Hz, 1H) m/e 365 1,3- 7.74-7.80 (m, 2H) 7.60-7.66 (m, 2H) 5.01 (d, J = 29.29 Hz, (M + H)⁺ dihydro-2H- 4H) 3.18 (d, J = 7.32 Hz, 2H) 2.08-2.21 (m, 1H) pyrrolo[3,4-c]pyridine- 1.45-1.72 (m, 6H) 1.21-1.29 (m, 2H) 2-carboxamide 739 N-{4-[(2- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.86 (s, 1H) (ESI(+)) thienylmethyl)carbamoyl]phenyl}- 8.76 (d, J = 5.80 Hz, 1H) 7.98 (d, J = 5.80 Hz, 1H) m/e 379 1,3- 7.79-7.85 (m, 2H) 7.63-7.68 (m, 2H) 7.37 (dd, J = 5.19, (M + H)⁺ dihydro-2H- 1.22 Hz, 1H) 7.03 (dd, J = 3.36, 1.22 Hz, 1H) pyrrolo[3,4-c]pyridine- 6.97 (dd, J = 5.19, 3.36 Hz, 1H) 5.00 (d, J = 27.16 Hz, 4H) 2-carboxamide 4.62 (s, 2H) 740 N-{4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1H) (ESI(+)) [methyl(tetrahydrofuran- 8.78 (d, J = 5.80 Hz, 1H) 8.02 (d, J = 5.80 Hz, 1H) m/e 381 2- 7.60 (d, J = 8.54 Hz, 2H) 7.34 (d, J = 4.58 Hz, 2H) 5.01 (d, (M + H)⁺ ylmethyl)carbamoyl]phenyl}- J = 30.21 Hz, 4H) 3.93-4.23 (m, 2H) 3.17-3.72 (m, 1,3-dihydro- 3H) 3.00 (s, 3H) 1.18-2.07 (m, 4H) 2H-pyrrolo[3,4- c]pyridine-2- carboxamide 741 N-{4-[(3- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1H) (ESI(+)) isopropoxypropyl)carbamoyl]phenyl}- 8.79 (d, J = 6.10 Hz, 1H) 8.03 (d, J = 5.80 Hz, 1H) m/e 383 1,3- 7.75-7.79 (m, 2H) 7.61-7.67 (m, 2H) 5.01 (d, J = 31.43 Hz, (M + H)⁺ dihydro-2H- 4H) 3.50-3.57 (m, 1H) 3.42 (t, J = 6.26 Hz, 2H) pyrrolo[3,4-c]pyridine- 3.31 (t, J = 7.02 Hz, 2H) 1.69-1.78 (m, 2H) 1.09 (d, 2-carboxamide J = 6.10 Hz, 6H) 742 N-{4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.89 (s, 1H) (ESI(+)) [benzyl(methyl)carbamoyl]phenyl}- 8.78 (d, J = 5.80 Hz, 1H) 8.03 (d, J = 5.80 Hz, 1H) m/e 387 1,3- 7.61 (s, 2H) 7.12-7.47 (m, 7H) 5.00 (d, J = 31.12 Hz, 4H) (M + H)⁺ dihydro-2H- 4.49-4.74 (m, 2H) 2.89 (s, 3H) pyrrolo[3,4-c]pyridine- 2-carboxamide 743 N-{4-[(3- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.84 (s, 1 (ESI(+)) aminobenzyl)carbamoyl]phenyl}- H) 8.73 (d, J = 5.80 Hz, 1H) 7.92 (d, J = 5.80 Hz, 1H) m/e 386 1,3- 7.83-7.86 (m, 2H) 7.64-7.68 (m, 2H) 7.43 (t, (M + H)⁺ dihydro-2H- J = 7.78 Hz, 1H) 7.30 (d, J = 7.93 Hz, 1H) 7.21 (s, 1H) pyrrolo[3,4-c]pyridine- 7.13-7.16 (m, 1H) 4.98 (d, J = 23.19 Hz, 4H) 4.49 (s, 2-carboxamide 2H) 744 N-{4-[(6- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.88 (s, 1H) (ESI(+)) methoxypyridin-3- 8.77 (d, J = 5.80 Hz, 1H) 8.48 (d, J = 2.44 Hz, 1H) m/e 390 yl)carbamoyl]phenyl}- 7.98-8.07 (m, 2H) 7.89-7.95 (m, 2H) 7.69-7.74 (m, 2 (M + H)⁺ 1,3-dihydro-2H- H) 6.87 (d, J = 8.85 Hz, 1H) 5.02 (d, J = 29.29 Hz, 4H) pyrrolo[3,4-c]pyridine- 3.83-3.88 (m, 3H) 2-carboxamide 745 N-{4-[(3- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.87 (s, 1H) (ESI(+)) isobutoxypropyl)carbamoyl]phenyl}- 8.76 (d, J = 5.80 Hz, 1H) 7.99 (d, J = 5.80 Hz, 1H) m/e 397 1,3- 7.74-7.80 (m, 2H) 7.61-7.66 (m, 2H) 5.00 (d, J = 28.07 Hz, (M + H)⁺ dihydro-2H- 4H) 3.43 (t, J = 6.26 Hz, 2H) 3.31 (t, J = 7.02 Hz, 2 pyrrolo[3,4-c]pyridine- H) 3.15 (d, J = 6.71 Hz, 2H) 1.71-1.81 (m, 3H) 2-carboxamide 0.86 (d, J = 6.71 Hz, 6H) 746 N-{4-[bis(2- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.88 (s, 1H) (ESI(+)) methoxyethyl)carbamoyl]phenyl}- 8.78 (d, J = 5.80 Hz, 1H) 8.02 (d, J = 6.10 Hz, 1H) m/e 399 1,3- 7.57-7.61 (m, 2H) 7.29-7.33 (m, 2H) 5.00 (d, J = 30.82 Hz, (M + H)⁺ dihydro-2H- 4H) 3.34-3.58 (m, 8H) 3.12-3.32 (m, 6H) pyrrolo[3,4-c]pyridine- 2-carboxamide 747 N-{4-[(4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.84 (s, 1H) (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- 8.74 (d, J = 5.80 Hz, 1H) 7.93 (d, J = 5.80 Hz, 1H) m/e 403 1,3- 7.79-7.83 (m, 2H) 7.62-7.66 (m, 2H) 7.23-7.30 (m, 2 (M + H)⁺ dihydro-2H- H) 6.86-6.93 (m, 2H) 4.98 (d, J = 24.11 Hz, 4H) pyrrolo[3,4-c]pyridine- 4.40 (s, 2H) 3.73 (s, 3H) 2-carboxamide 748 N-{4-[(3- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.87 (s, 1H) (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- 8.77 (d, J = 5.80 Hz, 1H) 8.00 (d, J = 6.10 Hz, 1H) m/e 403 1,3- 7.81-7.86 (m, 2H) 7.63-7.68 (m, 2H) 7.26 (t, J = 7.93 Hz, (M + H)⁺ dihydro-2H- 1H) 6.80-6.92 (m, 3H) 5.01 (d, J = 28.99 Hz, 4H) pyrrolo[3,4-c]pyridine- 4.44 (s, 2H) 3.74 (s, 3H) 2-carboxamide 749 N-(4-{[4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.88 (s, 1H) (ESI(+)) (trifluoromethyl)piperidin- 8.78 (d, J = 6.10 Hz, 1H) 8.02 (d, J = 6.10 Hz, 1H) m/e 419 1- 7.59-7.65 (m, 2H) 7.32-7.38 (m, 2H) 5.01 (d, J = 30.51 Hz, (M + H)⁺ yl]carbonyl}phenyl)- 4H) 4.55 (d, J = 47.91 Hz, 2H) 2.75-3.24 (m, 2 1,3-dihydro-2H- H) 2.59-2.68 (m, 1H) 1.87 (s, 2H) 1.34-1.49 (m, 2 pyrrolo[3,4-c]pyridine- H) 2-carboxamide 750 N-(4-{[4-(pyrazin-2- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.90 (s, 1H) (ESI(+)) yl)piperazin-1- 8.79 (d, J = 5.80 Hz, 1H) 8.32 (d, J = 1.22 Hz, 1H) m/e 430 yl]carbonyl}phenyl)- 8.13 (dd, J = 2.59, 1.37 Hz, 1H) 8.05 (d, J = 5.80 Hz, 1H) (M + H)⁺ 1,3-dihydro-2H- 7.88 (d, J = 2.75 Hz, 1H) 7.61-7.68 (m, 2H) pyrrolo[3,4-c]pyridine- 7.38-7.45 (m, 2H) 5.02 (d, J = 32.34 Hz, 4H) 2-carboxamide 3.44-3.76 (m, 8H) 751 N-{4-[(4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.88 (s, 1H) (ESI(+)) cyclohexylpiperazin-1- 8.78 (d, J = 6.10 Hz, 1H) 8.01 (d, J = 6.10 Hz, 1H) m/e 434 yl)carbonyl]phenyl}- 7.57-7.69 (m, 2H) 7.36-7.49 (m, 2H) 5.01 (d, J = 29.29 Hz, (M + H)⁺ 1,3-dihydro-2H- 4 H) 3.96 (s, 1H) 3.23-3.67 (m, 4H) pyrrolo[3,4-c]pyridine- 2.98-3.27 (m, 4H) 1.04-2.15 (m, 10H) 2-carboxamide 752 N-(4-{[2-(3,4- ¹H NMR (500 MHz, DMSO-D₂O) δ ppm 8.88 (s, 1H) (ESI(+)) dimethoxyphenyl)ethyl]carbamoyl}phenyl)- 8.77 (d, J = 5.80 Hz, 1H) 8.01 (d, J = 6.10 Hz, 1H) m/e 447 1,3-dihydro-2H- 7.73-7.80 (m, 2H) 7.58-7.68 (m, 2H) 6.84-6.89 (m, 2 (M + H)⁺ pyrrolo[3,4-c]pyridine- H) 6.77 (dd, J = 8.09, 1.98 Hz, 1H) 5.01 (d, J = 29.90 Hz, 2-carboxamide 4H) 3.96 (s, 1H) 3.70-3.73 (m, 6H) 3.46 (t, J = 7.32 Hz, 2H) 2.78 (t, J = 7.32 Hz, 2H) 770 N-(4-{[3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) (dimethylamino)propyl]carbamoyl}phenyl)- 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.70-7.78 (m, 2 m/e 368 1,3-dihydro-2H- H) 7.57-7.65 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ pyrrolo[3,4-c]pyridine- 4.80-4.87 (m, 4H) 3.30-3.34 (m, 2H) 2.28-2.40 (m, 2H) 2-carboxamide 2.17-2.21 (m, 6H) 1.61-1.75 (m, 2H) 771 N-(4-{[3-(morpholin- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) 4- 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.69-7.79 (m, 2 m/e 410 yl)propyl]carbamoyl}phenyl)- H) 7.57-7.64 (m, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ 1,3-dihydro- 4.80-4.87 (m, 4H) 3.54-3.62 (m, 4H) 3.31-3.34 (m, 2H) 2H-pyrrolo[3,4- 2.34-2.42 (m, 6H) 1.65-1.76 (m, 2H) c]pyridine-2- carboxamide 772 N-(4-{[4-(2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) aminoethyl)-1H- 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.71-7.76 (m, 2 m/e 377 imidazol-1- H) 7.57-7.66 (m, 2H) 7.52 (s, 1H) 7.41 (d, J = 5.19 Hz, (M + H)⁺ yl]carbonyl}phenyl)- 1H) 6.82 (s, 1H) 4.78-4.86 (m, 4H) 3.51 (t, 1,3-dihydro-2H- J = 7.32 Hz, 2H) 2.80 (t, J = 7.02 Hz, 2H) pyrrolo[3,4-c]pyridine- 2-carboxamide 773 N-[4-({4-[2-(2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) hydroxyethoxy)ethyl]piperazin- 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.56-7.62 (m, 2 m/e 440 1- H) 7.41 (d, J = 5.19 Hz, 1H) 7.27-7.33 (m, 2H) (M + H)⁺ yl}carbonyl)phenyl]- 4.79-4.87 (m, 4H) 3.40-3.60 (m, 10H) 2.53-2.57 (m, 2 1,3-dihydro-2H- H) 2.43-2.50 (m, 4H) pyrrolo[3,4-c]pyridine- 2-carboxamide 774 N-{4-[(3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) hydroxypropyl)carbamoyl]phenyl}- 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.71-7.78 (m, 2 m/e 341 1,3- H) 7.58-7.63 (m, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ dihydro-2H- 4.78-4.89 (m, 4H) 3.51 (t, J = 6.26 Hz, 2H) 3.34 (t, J = 6.87 Hz, pyrrolo[3,4-c]pyridine- 2H) 1.65-1.79 (m, 2H) 2-carboxamide 775 N-(4-{[4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) (dimethylamino)butyl]carbamoyl}phenyl)- 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.71-7.77 (m, 2 m/e 382 1,3-dihydro-2H- H) 7.58-7.64 (m, 2H) 7.42 (d, J = 4.88 Hz, 1H) (M + H)⁺ pyrrolo[3,4-c]pyridine- 4.79-4.88 (m, 4H) 3.27 (t, J = 6.87 Hz, 2H) 2.26-2.33 (m, 2-carboxamide 2H) 2.16 (s, 6H) 1.41-1.61 (m, 4H) 776 N-{4-[(pyridin-4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (ESI(+)) ylmethyl)carbamoyl]phenyl}- ppm 8.59 (s, 1H) 8.46-8.50 (m, 3H) 7.79-7.84 (m, m/e 374 1,3-dihydro- 2H) 7.62-7.67 (m, 2H) 7.42 (d, J = 4.88 Hz, 1H) (M + H)⁺ 2H-pyrrolo[3,4- 7.31 (d, J = 6.10 Hz, 2H) 4.84 (d, J = 7.02 Hz, 4H) c]pyridine-2- 4.49 (s, 2H) carboxamide 777 N-{4-[(pyridin-3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) ylmethyl)carbamoyl]phenyl}- 8.58 (s, 1H) 8.54 (d, J = 1.83 Hz, 1H) 8.48 (d, J = 5.19 Hz, m/e 374 1,3-dihydro- 1H) 8.43 (dd, J = 4.88, 1.53 Hz, 1H) (M + H)⁺ 2H-pyrrolo[3,4- 7.77-7.82 (m, 2H) 7.71-7.75 (m, 1H) 7.60-7.66 (m, 2H) c]pyridine-2- 7.41 (d, J = 5.19 Hz, 1H) 7.34 (dd, J = 7.93, 5.49 Hz, 1H) carboxamide 4.79-4.88 (m, 4H) 4.44-4.53 (m, 2H) 778 N-{4-[(pyrimidin-4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) ylmethyl)carbamoyl]phenyl}- 9.07 (d, J = 1.22 Hz, 1H) 8.70 (d, J = 5.19 Hz, 1H) m/e 375 1,3-dihydro- 8.59 (s, 1H) 8.49 (d, J = 4.88 Hz, 1H) 7.79-7.86 (m, 2H) (M + H)⁺ 2H-pyrrolo[3,4- 7.63-7.68 (m, 2H) 7.39-7.45 (m, 2H) c]pyridine-2- 4.81-4.87 (m, 4H) 4.56 (s, 2H) carboxamide 779 N-(4-{[2-(pyridin-3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) yl)ethyl]carbamoyl}phenyl)- 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 8.45 (d, J = 2.14 Hz, m/e 388 1,3-dihydro-2H- 1H) 8.39 (dd, J = 4.73, 1.68 Hz, 1H) (M + H)⁺ pyrrolo[3,4-c]pyridine- 7.69-7.73 (m, 2H) 7.64-7.68 (m, 1H) 7.58-7.62 (m, 2H) 2-carboxamide 7.42 (d, J = 4.88 Hz, 1H) 7.30 (dd, J = 7.93, 4.88 Hz, 1H) 4.81-4.85 (m, 4H) 3.52-3.57 (m, 2H) 2.87-2.92 (m, 2H) 780 N-(4-{[2-(4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ ppm (ESI(+)) methylpiperazin-1- 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.71-7.75 (m, 2 m/e 409 yl)ethyl]carbamoyl}phenyl)- H) 7.58-7.63 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 1,3-dihydro-2H- 4.81-4.86 (m, 4H) 3.38 (t, J = 6.87 Hz, 2H) 2.44-2.50 (m, pyrrolo[3,4-c]pyridine- 6H) 2.33-2.37 (m, 4H) 2.16 (s, 3H) 2-carboxamide 803 N-(4-{[(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.66 (s, 1H), (ESI(+)) methyloxetan-3- 8.61 (s, 1H), 8.51 (d, J = 5.0 Hz, 1H), 8.44 (t, J = 6.1 Hz, m/e 367 yl)methyl]carbamoyl}phenyl)- 1H), 7.84-7.76 (m, 2H), 7.71-7.63 (m, 2H), 7.44 (d, (M + H)⁺ 1,3-dihydro- J = 5.1 Hz, 1H), 4.87-4.80 (m, 4H), 4.48 (d, J = 5.7 Hz, 2H-pyrrolo[3,4- 2H), 4.20 (d, J = 5.7 Hz, 2H), 3.49-3.39 (m, 2H), c]pyridine-2- 1.25 (s, 3H) carboxamide 875 N-(4-{[(1,1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.72-8.56 (m, 2H), (ESI(+)) dioxidotetrahydrothiophen- 8.55-8.37 (m, 2H), 7.78 (d, J = 8.8 Hz, 2H), 7.67 (d, m/e 415 3- J = 8.8 Hz, 2H), 7.43 (t, J = 5.6 Hz, 1H), 4.83 (d, J = 4.3 Hz, (M + H)⁺ yl)methyl]carbamoyl}phenyl)- 4H), 3.50-3.29 (m, 1H), 3.27-2.99 (m, 3H), 1,3-dihydro- 2.88 (dt, J = 13.1, 7.2 Hz, 1H), 2.78-2.58 (m, 1H), 2H-pyrrolo[3,4- 2.33-2.11 (m, 1H), 1.97-1.72 (m, 1H) c]pyridine-2- carboxamide 880 N-{4-[(pyrrolidin-3- ¹H NMR (300 MHz, DMSO-d₆) δ 9.08 (s, 2H), (ESI(+)) ylmethyl)carbamoyl]phenyl}- 8.93 (d, J = 15.5 Hz, 2H), 8.82 (d, J = 5.8 Hz, 1H), 8.54 (t, m/e 366 1,3-dihydro- J = 5.8 Hz, 1H), 8.02 (d, J = 5.8 Hz, 1H), 7.81 (d, J = 8.6 Hz, (M + H)⁺ 2H-pyrrolo[3,4- 2H), 7.68 (d, J = 8.6 Hz, 2H), 5.06-4.95 (m, c]pyridine-2- 4H), 3.73-3.63 (m, 1H), 3.47-3.05 (m, 4H), carboxamide 3.02-2.80 (m, 1H), 2.07-1.92 (m, 1H), 1.67 (dq, J = 12.8, 8.1 Hz, 1H) 881 N-(4-{[(3S)- ¹H NMR (300 MHz, DMSO-d₆) δ 9.09 (s, 1H), (ESI(+)) pyrrolidin-3- 8.93 (d, J = 15.5 Hz, 1H), 8.82 (d, J = 5.8 Hz, 1H), 8.54 (t, m/e 366 ylmethyl]carbamoyl}phenyl)- J = 5.8 Hz, 1H), 8.03 (d, J = 5.8 Hz, 1H), 7.81 (d, J = 8.8 Hz, (M + H)⁺ 1,3-dihydro- 2H), 7.67 (d, J = 8.9 Hz, 2H), 5.00 (d, J = 19.2 Hz, 2H-pyrrolo[3,4- 4H), 3.69 (dq, J = 5.9, 4.4 Hz, 1H), c]pyridine-2- 3.52-3.44 (m, 1H), 3.35-3.07 (m, 4H), 2.90 (td, J = 13.7, 6.2 Hz, carboxamide 1H), 2.27 (s, 1H), 2.00 (td, J = 12.8, 7.4 Hz, 1H), 1.66 (dq, J = 16.3, 8.2 Hz, 1H) 882 N-(4-{[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 9.59 (s, 1H), (ESI(+)) methylpyrrolidin-3- 8.35 (s, 1H), 7.56-7.49 (m, 2H), 7.41-7.23 (m, 5H), m/e 380 yl)methyl]carbamoyl}phenyl)- 7.13 (s, 1H), 7.10 (s, 1H), 6.92 (dd, J = 8.3, 2.6 Hz, 1H), (M + H)⁺ 1,3-dihydro- 6.89-6.79 (m, 2H), 4.76 (s, 4H), 4.36 (s, 2H), 3.73 (s, 2H-pyrrolo[3,4- 3H) c]pyridine-2- carboxamide 884 N-(4-{[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.66-8.59 (m, 2H), (ESI(+)) methylpiperidin-4- 8.50 (d, J = 5.0 Hz, 1H), 8.26 (t, J = 5.8 Hz, 1H), m/e 394 yl)methyl]carbamoyl}phenyl)- 7.81-7.73 (m, 2H), 7.68-7.61 (m, 2H), 7.44 (d, J = 5.1 Hz, (M + H)⁺ 1,3-dihydro- 1H), 4.86-4.75 (m, 4H), 3.12 (t, J = 6.2 Hz, 2H), 2H-pyrrolo[3,4- 2.77-2.69 (m, 2H), 2.12 (s, 3H), 1.78 (td, J = 11.5, c]pyridine-2- 2.4 Hz, 2H), 1.63 (dd, J = 12.5, 2.9 Hz, 2H), carboxamide 1.54-1.40 (m, 1H), 1.25-1.08 (m, 2H) 922 N-[4-({[(3R)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.66 (s, 1H), (ESI(+)) isobutyrylpyrrolidin-3- 8.61 (s, 1H), 8.50 (d, J = 5.0 Hz, 1H), 8.41 (t, J = 5.3 Hz, m/e 436 yl]methyl}carbamoyl)phenyl]- 1H), 7.82-7.74 (m, 2H), 7.70-7.62 (m, 2H), 7.44 (d, (M + H)⁺ 1,3-dihydro- J = 5.1 Hz, 1H), 4.84-4.74 (m, 4H), 3.58 (dd, J = 17.0, 2H-pyrrolo[3,4- 9.7 Hz, 1H), 3.44 (dt, J = 22.7, 9.2 Hz, 1H), c]pyridine-2- 3.28-2.93 (m, 2H), 2.64 (pd, J = 6.7, 3.2 Hz, 1H), carboxamide 2.08-1.83 (m, 1H), 1.78-1.45 (m, 1H), 1.29-1.24 (m, 3H), 1.08-0.91 (m, 6H) 923 N-[4-({[(3R)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.68-8.59 (m, 2H), (ESI(+)) benzoylpyrrolidin-3- 8.49 (t, J = 5.1 Hz, 1H), 8.47-8.41 (m, 1H), m/e 470 yl]methyl}carbamoyl)phenyl]- 8.40-8.28 (m, 1H), 7.85-7.76 (m, 1H), 7.76-7.58 (m, (M + H)⁺ 1,3-dihydro- 3H), 7.54-7.46 (m, 2H), 7.42 (t, J = 7.6 Hz, 3H), 2H-pyrrolo[3,4- 4.80 (d, J = 15.4 Hz, 4H), 3.68-3.55 (m, 1H), c]pyridine-2- 3.53-3.36 (m, 1H), 3.20 (ddd, J = 9.8, 7.1, 5.7 Hz, 1H), carboxamide 2.06-1.87 (m, 2H), 1.76-1.58 (m, 2H), 1.31-1.18 (m, 2H) 924 N-[4-({[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.63 (d, J = 12.1 Hz, (ESI(+)) (tetrahydrofuran-3- 2H), 8.50 (d, J = 5.0 Hz, 1H), 8.41 (s, 1H), m/e 464 ylcarbonyl)pyrrolidin- 7.78 (d, J = 8.8 Hz, 2H), 7.66 (d, J = 8.1 Hz, 2H), 7.44 (d, J = 5.0 Hz, (M + H)⁺ 3- 1H), 4.83 (d, J = 4.3 Hz, 4H), 3.88 (t, J = 8.1 Hz, yl]methyl}carbamoyl)phenyl]- 1H), 3.77-3.59 (m, 4H), 3.52-3.40 (m, 1H), 1,3-dihydro- 3.27-3.06 (m, 2H), 2.40 (dd, J = 13.9, 6.8 Hz, 1H), 2H-pyrrolo[3,4- 2.07-1.90 (m, 3H), 1.78-1.55 (m, 1H), 1.23 (dd, J = 9.7, c]pyridine-2- 6.6 Hz, 1H) carboxamide 925 N-[4-({[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.66 (s, 1H), (ESI(+)) (methylsulfonyl)pyrrolidin- 8.62 (s, 1H), 8.51 (d, J = 5.0 Hz, 1H), 8.42 (t, J = 5.7 Hz, m/e 444 3- 1H), 7.82-7.74 (m, 2H), 7.70-7.63 (m, 2H), 7.44 (d, (M + H)⁺ yl]methyl}carbamoyl)phenyl]- J = 5.1 Hz, 1H), 4.86-4.79 (m, 4H), 3.25-3.11 (m, 1,3-dihydro- 2H), 3.02 (dd, J = 10.0, 6.7 Hz, 1H), 2.90 (s, 3H), 2H-pyrrolo[3,4- 2.06-1.89 (m, 2H), 1.75-1.59 (m, 2H), 1.28-1.20 (m, c]pyridine-2- 2H) carboxamide 939 N-[4-({[1-(morpholin- ¹H NMR (300 MHz, DMSO-d₆) δ 9.35 (s, 1H), (ESI(+)) 4- 8.77 (s, 1H), 8.72 (s, 1H), 8.60 (d, J = 5.3 Hz, 2H), 7.84 (d, m/e 451 yl)cyclopentyl]methyl}carbamoyl)phenyl]- J = 8.8 Hz, 2H), 7.71 (d, J = 8.8 Hz, 2H), 7.61 (d, J = 5.2 Hz, (M + H)⁺ 1,3-dihydro-2H- 1H), 4.88 (s, 4H), 4.03 (d, J = 11.7 Hz, 3H), pyrrolo[3,4-c]pyridine- 3.79-3.57 (m, 5H), 3.51 (d, J = 11.5 Hz, 2H), 2-carboxamide 3.38 (d, J = 9.6 Hz, 2H), 1.95 (d, J = 6.9 Hz, 4H), 1.74 (s, 4H) 969 N-(4-{[(1S)-1-(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.66 (s, 1H), (ESI(+)) fluorophenyl)-2- 8.62 (s, 1H), 8.50 (d, J = 9.6 Hz, 2H), 7.87-7.80 (m, 2H), m/e 421 hydroxyethyl]carbamoyl}phenyl)- 7.71-7.64 (m, 2H), 7.47-7.38 (m, 3H), 7.14 (t, J = 8.7 Hz, (M + H)⁺ 1,3- 2H), 5.12-5.00 (m, 1H), 4.91 (t, J = 5.8 Hz, dihydro-2H- 1H), 4.83 (d, J = 4.4 Hz, 4H), 3.76-3.57 (m, 2H) pyrrolo[3,4-c]pyridine- 2-carboxamide 970 N-(4-{[(1S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.63 (d, J = 10.4 Hz, (ESI(+)) hydroxy-1-(4- 2H), 8.49 (t, J = 7.8 Hz, 1H), 8.41 (d, J = 8.2 Hz, m/e 433 methoxyphenyl)ethyl]carbamoyl}phenyl)- 1H), 7.83 (d, J = 8.8 Hz, 2H), 7.67 (d, J = 8.8 Hz, 2H), (M + H)⁺ 1,3- 7.44 (d, J = 5.1 Hz, 1H), 7.36-7.25 (m, 2H), dihydro-2H- 6.92-6.82 (m, 2H), 5.01 (dd, J = 13.7, 7.9 Hz, 1H), 4.84 (t, J = 5.7 Hz, pyrrolo[3,4-c]pyridine- 4H), 3.72 (s, 3H), 3.70-3.57 (m, 3H) 2-carboxamide 971 N-[4-({[3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.67 (s, 1H), (ESI(+)) (hydroxymethyl)oxetan- 8.62 (s, 1H), 8.51 (d, J = 5.1 Hz, 1H), 8.49-8.41 (m, 1H), m/e 383 3- 7.83-7.76 (m, 2H), 7.71-7.64 (m, 2H), 7.44 (d, J = 5.1 Hz, (M + H)⁺ yl]methyl}carbamoyl)phenyl]- 1H), 4.93-4.86 (m, 1H), 4.84 (t, J = 7.0 Hz, 1,3-dihydro- 2H), 4.40 (d, J = 5.9 Hz, 2H), 4.29 (d, J = 5.8 Hz, 2H), 2H-pyrrolo[3,4- 3.58 (d, J = 5.6 Hz, 2H), 3.51 (d, J = 6.0 Hz, 2H) c]pyridine-2- carboxamide 972 N-(4-{[(1S)-1-(1,3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.70-8.57 (m, 2H), (ESI(+)) benzodioxol-5-yl)-2- 8.54-8.46 (m, 1H), 8.43-8.27 (m, 1H), m/e 447 hydroxyethyl]carbamoyl}phenyl)- 7.87-7.77 (m, 2H), 7.67 (d, J = 8.8 Hz, 2H), 7.49-7.38 (m, 1H), (M + H)⁺ 1,3- 6.99 (s, 1H), 6.84 (d, J = 0.8 Hz, 2H), 5.96 (dd, J = 2.5, dihydro-2H- 0.8 Hz, 2H), 5.04-4.94 (m, 1H), 4.89-4.75 (m, pyrrolo[3,4-c]pyridine- 4H), 3.73-3.53 (m, 2H) 2-carboxamide 1055 N-[4-(1,7- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm 8.44 (d, J = 20.6 Hz, (ESI(+)) diazaspiro[4.4]non-7- 1H), 7.88 (t, J = 10.7 Hz, 3H), m/e 392 ylcarbonyl)phenyl]- 7.69-7.57 (m, 3H), 4.22 (d, J = 12.3 Hz, 1H), 3.93 (dt, J = 11.3, (M + H)⁺ 1,3-dihydro-2H- 8.0 Hz, 2H), 3.83-3.64 (m, 3H), 3.59-3.46 (m, 3H), pyrrolo[3,4-c]pyridine- 3.45-3.31 (m, 1H), 2.71-2.46 (m, 1H), 2-carboxamide 2.12-1.80 (m, 8H) 1056 N-[4-(2,7- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm 8.55 (dd, J = 10.2, (ESI(+)) diazaspiro[4.5]dec-2- 5.1 Hz, 2H), 7.99-7.83 (m, 2H), 7.70-7.61 (m, m/e 406 ylcarbonyl)phenyl]- 2H), 7.10 (d, J = 4.9 Hz, 1H), 4.99-4.79 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 3.74-3.59 (m, 4H), 3.28-3.10 (m, 4H), pyrrolo[3,4-c]pyridine- 2.13-1.91 (m, 1H), 1.91-1.72 (m, 2H), 1.71-1.60 (m, 1H), 2-carboxamide 1.64-1.45 (m, 2H) 1057 N-[4-(2,6- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[4.5]dec-2- 8.58-8.47 (m, 2H), 7.85 (t, J = 24.8 Hz, 2H), 7.67-7.57 (m, m/e 406 ylcarbonyl)phenyl]- 2H), 7.10 (d, J = 4.9 Hz, 1H), 4.91-4.74 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 4.30 (d, J = 12.6 Hz, 1H), 3.98-3.72 (m, 2H), pyrrolo[3,4-c]pyridine- 3.68-3.58 (m, 1H), 3.27-3.05 (m, 2H), 2.61-2.45 (m, 2-carboxamide 1H), 2.16-1.92 (m, 1H), 1.92-1.77 (m, 2H), 1.72-1.19 (m, 4H) 1058 N-[4-(2,7- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[4.5]dec-7- 8.60-8.49 (m, 2H), 8.09-7.83 (m, 2H), 7.53-7.42 (m, 3H), m/e 406 ylcarbonyl)phenyl]- 5.06-4.76 (m, 4H), 3.78-3.57 (m, 3H), (M + H)⁺ 1,3-dihydro-2H- 3.48-3.23 (m, 4H), 2.08-1.91 (m, 1H), 1.91-1.76 (m, 1H), pyrrolo[3,4-c]pyridine- 1.76-1.65 (m, 1H), 1.61 (dt, J = 23.9, 13.1 Hz, 1H), 2-carboxamide 1.56-1.34 (m, 2H) 1059 N-[4-(2,9- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[5.5]undec- 8.62-8.46 (m, 2H), 7.85 (dd, J = 43.4, 8.8 Hz, 2H), m/e 420 2-ylcarbonyl)phenyl]- 7.52-7.43 (m, 2H), 7.10 (d, J = 4.9 Hz, 1H), 3.90-3.70 (m, (M + H)⁺ 1,3-dihydro-2H- 1H), 3.60-3.43 (m, 3H), 3.41-3.25 (m, 1H), pyrrolo[3,4-c]pyridine- 3.24-3.03 (m, 4H), 1.89-1.56 (m, 4H), 1.54-1.31 (m, 4H) 2-carboxamide 1060 N-[4-(2,8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm 8.56 (dd, J = 9.9, (ESI(+)) diazaspiro[5.5]undec- 4.6 Hz, 2H), 8.12-7.80 (m, 2H), 7.52-7.43 (m, m/e 420 2-ylcarbonyl)phenyl]- 3H), 4.90-4.83 (m, 6H), 3.67-3.55 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 3.49-3.37 (m, 2H), 3.41-3.23 (m, 4H), 1.99-1.61 (m, pyrrolo[3,4-c]pyridine- 4H), 1.47 (d, J = 10.4 Hz, 4H) 2-carboxamide 1061 N-[4-(1,8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[5.5]undec- 8.60-8.44 (m, 2H), 7.86 (t, J = 25.2 Hz, 2H), 7.54 (t, J = 6.9 Hz, m/e 420 8-ylcarbonyl)phenyl]- 2 H), 7.10 (d, J = 4.9 Hz, 1H), 4.14 (d, J = 13.5 Hz, (M + H)⁺ 1,3-dihydro-2H- 1H), 4.02 (d, J = 13.5 Hz, 1H), 3.59 (dd, J = 11.5, 6.5 Hz, pyrrolo[3,4-c]pyridine- 1H), 3.48-3.33 (m, 1H), 3.36-3.13 (m, 2H), 2-carboxamide 2.23 (ddd, J = 13.3, 8.9, 4.3 Hz, 1H), 1.96-1.82 (m, 2H), 1.83-1.65 (m, 4H), 1.69-1.44 (m, 4H) 1062 N-[4-(1,8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm 8.50 (dd, J = 43.2, (ESI(+)) diazaspiro[4.6]undec- 14.6 Hz, 2H), 7.98-7.82 (m, 2H), m/e 420 8-ylcarbonyl)phenyl]- 7.52-7.41 (m, 2H), 7.10 (d, J = 4.9 Hz, 1H), 3.95-3.75 (m, 1H), (M + H)⁺ 1,3-dihydro-2H- 3.67 (d, J = 9.3 Hz, 2H), 3.51-3.37 (m, 6H), pyrrolo[3,4-c]pyridine- 2.52-2.33 (m, 1H), 2.25-2.11 (m, 2H), 2.12-1.99 (m, 2-carboxamide 1H), 2.03-1.83 (m, 6H), 1.66 (d, J = 41.1 Hz, 1H) 1063 N-{4-[(1-oxa-8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) azaspiro[4.5]dec-2- 8.61-8.44 (m, 2H), 8.18-8.03 (m, 2H), 7.98-7.81 (m, 2H), m/e 436 ylmethyl)carbamoyl]phenyl}- 7.10 (d, J = 4.9 Hz, 1H) 4.89-4.79 (m, 6H), 4.28 (dt, (M + H)⁺ 1,3-dihydro- J = 12.4, 6.2 Hz, 1H), 3.80-3.64 (m, 2H), 3.51 (s, 2H-pyrrolo[3,4- 1H), 3.45-3.25 (m, 4H), 2.12-1.89 (m, 2H), c]pyridine-2- 1.87-1.48 (m, 4H) carboxamide 1064 N-[4-(1-oxa-8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm 8.44 (d, J = 20.6 Hz, (ESI(+)) azaspiro[4.5]dec-3- 1H), 7.88 (t, J = 10.7 Hz, 3H), m/e 422 ylcarbamoyl)phenyl]- 7.69-7.57 (m, 3H), 4.22 (d, J = 12.3 Hz, 1H), 3.93 (dt, J = 11.3, (M + H)⁺ 1,3-dihydro-2H- 8.0 Hz, 2H), 3.83-3.64 (m, 3H), 3.59-3.46 (m, 3H), pyrrolo[3,4-c]pyridine- 3.45-3.31 (m, 1H), 2.71-2.46 (m, 1H), 2-carboxamide 2.12-1.80 (m, 8H) 1065 N-{4-[(2-oxa-9- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) azaspiro[5.5]undec-3- 8.56-8.44 (m, 2H), 8.26-8.00 (m, 3H), 7.87 (dd, J = 40.3, 8.7 Hz, m/e 450 ylmethyl)carbamoyl]phenyl}- 2H), 3.99-3.70 (m, 2H), 3.66-3.56 (m, 2H), (M + H)⁺ 1,3-dihydro- 3.51 (s, 1H), 3.35-3.16 (m, 4H), 3.10 (d, J = 11.5 Hz, 2H-pyrrolo[3,4- 1H), 2.09-1.82 (m, 2H), 1.83-1.68 (m, 1H), c]pyridine-2- 1.61-1.36 (m, 4H), 1.33-1.05 (m, 1H) carboxamide 1066 N-[4-(1-oxa-4,8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[5.5]undec- 8.62-8.46 (m, 2H), 7.86 (dd, J = 52.3, 8.6 Hz, 3H), 7.56 (d, J = 15.9 Hz, m/e 422 4-ylcarbonyl)phenyl]- 2H), 4.94-4.73 (m, 5H), 3.81-3.52 (m, (M + H)⁺ 1,3-dihydro-2H- 6H), 3.37 (d, J = 12.4 Hz, 1H), 3.17-2.87 (m, 2H), pyrrolo[3,4-c]pyridine- 2.13-1.83 (m, 2H), 1.63-1.24 (m, 2H) 2-carboxamide 1067 N-[4-(1,8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[4.5]dec-1- 8.59-8.45 (m, 2H), 7.96-7.80 (m, 2H), 7.59-7.52 (m, 2H), m/e 406 ylcarbonyl)phenyl]- 7.10 (d, J = 4.9 Hz, 1H), 4.87 (d, J = 6.5 Hz, 6H), (M + H)⁺ 1,3-dihydro-2H- 3.54 (dt, J = 13.2, 4.8 Hz, 4H), 3.41 (dd, J = 9.0, 4.4 Hz, pyrrolo[3,4-c]pyridine- 2H), 3.28-3.12 (m, 2H), 2.03-1.86 (m, 2H), 2-carboxamide 1.74-1.46 (m, 4H) 1068 N-[4-(1,8- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm 8.50 (dd, J = 44.5, (ESI(+)) diazaspiro[4.5]dec-8- 13.2 Hz, 2H), 7.88 (d, J = 8.5 Hz, 2H), 7.50 (d, J = 8.6 Hz, m/e 406 ylcarbonyl)phenyl]- 2H), 7.10 (d, J = 4.9 Hz, 1H), (M + H)⁺ 1,3-dihydro-2H- 4.14-3.91 (m, 2H), 3.66-3.34 (m, 6H), 2.43 (s, 1H), pyrrolo[3,4-c]pyridine- 2.23-2.05 (m, 2H), 2.05-1.66 (m, 8H) 2-carboxamide 1069 N-[4-(1,7- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[3.5]non-7- 8.59-8.43 (m, 2H), 7.90 (d, J = 8.5 Hz, 2H), 7.48 (t, J = 13.3 Hz, m/e 392 ylcarbonyl)phenyl]- 3H), 4.90 (dd, J = 29.4, 12.8 Hz, 4H), 4.01 (d, J = 47.2 Hz, (M + H)⁺ 1,3-dihydro-2H- 2H), 3.61 (t, J = 5.7 Hz, 2H), 3.51 (s, 2H), 3.37 (t, pyrrolo[3,4-c]pyridine- J = 7.4 Hz, 2H), 2.61 (t, J = 7.3 Hz, 2H), 2.10 (s, 2H) 2-carboxamide 1070 N-[4-(1,6- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm 8.56 (d, J = 6.6 Hz, (ESI(+)) diazaspiro[3.5]non-1- 2H), 8.05-7.86 (m, 2H), 7.82-7.62 (m, 2H), m/e 392 ylcarbonyl)phenyl]- 7.10 (d, J = 4.9 Hz, 1H), 4.98-4.75 (m, 4H), 4.27 (td, (M + H)⁺ 1,3-dihydro-2H- J = 8.9, 6.8 Hz, 1H), 3.96 (ddd, J = 25.0, 14.5, 9.4 Hz, pyrrolo[3,4-c]pyridine- 3H), 3.51 (d, J = 6.5 Hz, 1H), 3.44 (t, J = 9.6 Hz, 1H), 2-carboxamide 3.23 (tdd, J = 12.8, 11.1, 4.3 Hz, 2H), 2.58-2.45 (m, 1H), 2.39-2.19 (m, 1H), 1.97 (ddd, J = 11.3, 9.0, 5.2 Hz, 2H), 1.89-1.63 (m, 2H) 1071 N-[4-(2,5- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) diazaspiro[3.5]non-2- 8.59-8.44 (m, 2H), 7.90 (d, J = 8.7 Hz, 2H), 7.84-7.67 (m, 2H), m/e 392 ylcarbonyl)phenyl]- 7.10 (d, J = 4.9 Hz, 1H), 4.89 (dd, J = 31.4, 12.8 Hz, (M + H)⁺ 1,3-dihydro-2H- 4H), 4.38 (d, J = 9.7 Hz, 2H), 4.29-4.03 (m, 2H), pyrrolo[3,4-c]pyridine- 3.51 (s, 1H), 3.12-2.82 (m, 2H), 2.01-1.69 (m, 2H), 2-carboxamide 1.62-1.22 (m, 4H) 1072 N-[4-(5-oxa-2- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) azaspiro[3.4]oct-2- 8.60-8.44 (m, 3H), 7.99-7.85 (m, 2H), 7.85-7.74 (m, 2H), m/e 379 ylcarbonyl)phenyl]- 7.10 (d, J = 4.9 Hz, 1H), 4.98-4.74 (m, 4H), (M + H)⁺ 1,3-dihydro-2H- 4.41-4.24 (m, 3H), 4.19 (dd, J = 9.6, 1.2 Hz, 2H), pyrrolo[3,4-c]pyridine- 3.85-3.61 (m, 2H), 1.92 (t, J = 7.3 Hz, 2H), 1.80-1.54 (m, 2-carboxamide 2H) 1073 N-[4-(6-oxa-2- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) azaspiro[3.5]non-2- 8.58-8.43 (m, 2H), 7.91 (dd, J = 21.0, 8.7 Hz, 2H), 7.85 (t, J = 7.0 Hz, m/e 393 ylcarbonyl)phenyl]- 2H), 7.11 (d, J = 4.9 Hz, 1H), 4.88 (t, J = 13.2 Hz, (M + H)⁺ 1,3-dihydro-2H- 4H), 4.04-3.91 (m, 2H), 3.91-3.76 (m, 2H), pyrrolo[3,4-c]pyridine- 3.62-3.54 (m, 2H), 3.54-3.36 (m, 3H), 2-carboxamide 1.77-1.52 (m, 2H), 1.52-1.27 (m, 2H) 1074 N-[4-(hexahydro-5H- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) furo[2,3-c]pyrrol-5- 8.57-8.46 (m, 2H), 7.98-7.76 (m, 2H), 7.69-7.57 (m, 2H), m/e 379 ylcarbonyl)phenyl]- 7.10 (s, 1H), 4.86 (dd, J = 17.1, 10.2 Hz, 4H), 4.39 (t, (M + H)⁺ 1,3-dihydro-2H- J = 5.6 Hz, 1H), 3.98-3.81 (m, 2H), 3.74-3.54 (m, pyrrolo[3,4-c]pyridine- 4H), 3.56-3.41 (m, 1H), 2.78-2.51 (m, 1H), 2-carboxamide 2.07-1.72 (m, 1H), 1.73-1.36 (m, 1H) 1075 N-[4-(tetrahydro-1H- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) furo[3,4-c]pyrrol- 8.59-8.46 (m, 2H), 7.90 (d, J = 8.6 Hz, 2H), 7.68-7.58 (m, 2H), m/e 379 5(3H)- 7.10 (d, J = 5.0 Hz, 1H), 4.87 (dd, J = 16.8, 9.9 Hz, (M + H)⁺ ylcarbonyl)phenyl]- 4H), 3.86-3.64 (m, 4H), 3.64-3.40 (m, 5H), 1,3-dihydro-2H- 2.86-2.58 (m, 2H) pyrrolo[3,4-c]pyridine- 2-carboxamide 1076 N-[4- ¹H NMR (400 MHz, Pyridine-d₅) δ ppm (ESI(+)) (hexahydrofuro[3,4- 8.62-8.45 (m, 2H), 8.01-7.80 (m, 2H), 7.57-7.52 (m, 2H), m/e 393 c]pyridin-5(3H)- 7.10 (d, J = 5.1 Hz, 1H), 4.91-4.78 (m, 4H), (M + H)⁺ ylcarbonyl)phenyl]- 3.83-3.69 (m, 2H), 3.74-3.55 (m, 6H), 3.45-3.26 (m, 1,3-dihydro-2H- 1H), 2.37-2.17 (m, 2H), 1.72-1.35 (m, 2H) pyrrolo[3,4-c]pyridine- 2-carboxamide 1120 N-(4-{[3-(5-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 1H-pyrazol-1- 8.47 (d, J = 4.9 Hz, 1H), 7.80 (d, J = 7.7 Hz, 1H), m/e 405 yl)propyl]carbamoyl}phenyl)- 7.78-7.70 (m, 2H), 7.70-7.54 (m, 2H), 7.42-7.09 (m, (M + H)⁺ 5,7-dihydro- 2H), 6.01 (d, J = 0.8 Hz, 1H), 4.81 (d, J = 11.5 Hz, 6H-pyrrolo[3,4- 4H), 4.08 (t, J = 7.0 Hz, 2H), 3.32-3.27 (m, 2H), b]pyridine-6- 2.25 (s, 3H), 2.12-1.94 (m, 2H) carboxamide 1121 N-(4-{[2-(4-chloro- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 1H-pyrazol-1- 8.52-8.38 (m, 1H), 7.87-7.76 (m, 2H), 7.73-7.66 (m, m/e 411 yl)ethyl]carbamoyl}phenyl)- 2H), 7.66-7.55 (m, 2H), 7.54-7.39 (m, 1H), (M + H)⁺ 5,7-dihydro-6H- 7.38-7.22 (m, 1H), 4.95-4.64 (m, 4H), 4.28 (dd, J = 8.0, pyrrolo[3,4-b]pyridine- 4.5 Hz, 2H), 3.79-3.50 (m, 2H) 6-carboxamide 1122 N-(4-{[1-(3,5- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.47 (t, (ESI(+)) dimethyl-1H-pyrazol- J = 9.6 Hz, 1H), 7.91-7.78 (m, 1H), 7.79-7.68 (m, m/e 419 1-yl)propan-2- 2H), 7.68-7.57 (m, 2H), 7.38-7.31 (m, 1H), 4.82 (d, (M + H)⁺ yl]carbamoyl}phenyl)- J = 8.8 Hz, 4H), 4.37 (h, J = 6.7 Hz, 1H), 5,7-dihydro-6H- 4.24-3.93 (m, 2H), 2.89-2.68 (m, 1H), 2.63-2.42 (m, 2H), pyrrolo[3,4-b]pyridine- 2.13 (s, 3H), 1.96 (s, 1H), 1.27-1.02 (m, 3H) 6-carboxamide 1123 N-(4-{[2-methyl-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (morpholin-4- 8.47 (d, J = 4.8 Hz, 1H), 7.81 (dd, J = 10.0, 8.1 Hz, 3H), m/e 438 yl)butyl]carbamoyl}phenyl)- 7.75-7.60 (m, 2H), 7.46-7.25 (m, 1H), 4.81 (d, J = 12.8 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 3.92 (s, 4H), 3.40 (s, 3H), 2.85 (dd, J = 84.9, pyrrolo[3,4-b]pyridine- 29.4 Hz, 2H), 2.57-2.38 (m, 3H), 1.92 (d, J = 35.3 Hz, 6-carboxamide 1H), 1.87-1.66 (m, 2H), 1.02 (t, J = 7.4 Hz, 3H) 1124 N-{4-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- 8.55-8.39 (m, 1H), 7.98-7.71 (m, 3H), 7.67-7.52 (m, m/e 403 5,7- 2H), 7.36-7.29 (m, 1H), 7.29-7.17 (m, 2H), (M + H)⁺ dihydro-6H- 6.98-6.73 (m, 2H), 4.90-4.60 (m, 4H), 4.38 (d, J = 17.5 Hz, pyrrolo[3,4-b]pyridine- 2H), 3.74 (d, J = 3.2 Hz, 3H) 6-carboxamide 1125 N-(4-{[3-(morpholin- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 4- 8.57-8.35 (m, 1H), 7.89-7.72 (m, 3H), 7.72-7.54 (m, m/e 410 yl)propyl]carbamoyl}phenyl)- 2H), 7.33 (dd, J = 7.7, 5.0 Hz, 1H), 4.81 (d, J = 11.8 Hz, (M + H)⁺ 5,7-dihydro- 4H), 3.86 (s, 4H), 3.47-3.34 (m, 2H), 6H-pyrrolo[3,4- 3.24-3.04 (m, 2H), 2.12-1.78 (m, 2H) b]pyridine-6- carboxamide 1126 N-[4-({4-[2-(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) hydroxyethoxy)ethyl]piperazin- 8.46 (dd, J = 12.7, 2.9 Hz, 1H), 7.80 (d, J = 7.7 Hz, 1H), m/e 440 1- 7.73-7.55 (m, 2H), 7.49-7.35 (m, 2H), (M + H)⁺ yl}carbonyl)phenyl]- 7.35-7.25 (m, 1H), 4.81 (d, J = 11.4 Hz, 4H), 3.90-3.71 (m, 5,7-dihydro-6H- 6H), 3.66-3.48 (m, 5H), 3.37 (d, J = 5.2 Hz, 5H), pyrrolo[3,4-b]pyridine- 2.88 (d, J = 53.2 Hz, 4H), 1.96 (s, 2H) 6-carboxamide 1127 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) carbamoylbenzyl)carbamoyl]phenyl}- 8.46 (d, J = 4.3 Hz, 1H), 7.84-7.73 (m, 3H), m/e 416 5,7- 7.73-7.59 (m, 2H), 7.48 (d, J = 7.4 Hz, 1H), 7.44-7.37 (m, 2H), (M + H)⁺ dihydro-6H- 7.37-7.20 (m, 2H), 4.81 (d, J = 12.6 Hz, 4H), 4.63 (s, pyrrolo[3,4-b]pyridine- 2H) 6-carboxamide 1128 N-{4-[bis(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxyethyl)carbamoyl]phenyl}- 8.65-8.37 (m, 1H), 7.78 (dd, J = 40.2, 6.3 Hz, 1H), m/e 399 5,7-dihydro- 7.68-7.53 (m, 2H), 7.42-7.31 (m, 1H), 7.32-7.20 (m, (M + H)⁺ 6H-pyrrolo[3,4- 2H), 4.85 (t, J = 26.3 Hz, 4H), 3.67-3.41 (m, 9H), b]pyridine-6- 3.28 (t, J = 8.4 Hz, 6H), 3.06-2.71 (m, 2H), 2.01 (d, J = 38.9 Hz, carboxamide 1H) 1129 N-{4-[(1-amino-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) oxohexan-2- 8.59-8.22 (m, 1H), 7.89-7.75 (m, 3H), 7.70-7.54 (m, m/e 394 yl)carbamoyl]phenyl}- 2H), 7.37 (dd, J = 7.7, 5.0 Hz, 1H), 4.83 (d, J = 8.7 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 4.41 (dd, J = 8.6, 5.5 Hz, 1H), pyrrolo[3,4-b]pyridine- 3.11-2.72 (m, 1H), 2.53-2.31 (m, 1H), 1.90-1.56 (m, 2H), 6-carboxamide 1.48-1.22 (m, 4H), 1.11-0.77 (m, 3H) 1130 N-(4-{[2-(3,4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dimethoxyphenyl)ethyl]carbamoyl}phenyl)- 8.55-8.34 (m, 1H), 7.87-7.75 (m, 1H), 7.76-7.67 (m, m/e 447 5,7-dihydro-6H- 2H), 7.67-7.52 (m, 2H), 7.45-7.26 (m, 1H), (M + H)⁺ pyrrolo[3,4-b]pyridine- 6.94-6.79 (m, 2H), 6.77 (dd, J = 8.1, 2.0 Hz, 1H), 6-carboxamide 4.90-4.61 (m, 4H), 3.73 (d, J = 2.9 Hz, 6H), 3.63-3.35 (m, 2H), 2.87-2.66 (m, 2H) 1131 N-(4-{[4-(pyrazin-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) yl)piperazin-1- 8.31-8.22 (m, 1H), 8.12-8.04 (m, 1H), 7.90-7.59 (m, m/e 430 yl]carbonyl}phenyl)- 4H), 7.43-7.30 (m, 3H), 4.87-4.75 (m, 4H), (M + H)⁺ 5,7-dihydro-6H- 3.69-3.60 (m, 8H) pyrrolo[3,4-b]pyridine- 6-carboxamide 1132 Nalpha-{4-[(5,7- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dihydro-6H- 8.57-8.27 (m, 1H), 7.83-7.74 (m, 1H), 7.74-7.64 (m, m/e 430 pyrrolo[3,4-b]pyridin- 2H), 7.64-7.54 (m, 2H), 7.39-7.20 (m, 5H), (M + H)⁺ 6- 7.20-7.09 (m, 1H), 4.88-4.73 (m, 4H), 4.73-4.58 (m, ylcarbonyl)amino]benzoyl}- 1H), 3.22-3.11 (m, 1H), 3.11-2.92 (m, 1H) L- phenylalaninamide 1133 N-(4-{[(2R)-1-amino- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 4-methyl-1-oxopentan- 8.61-8.35 (m, 1H), 7.96-7.73 (m, 3H), 7.71-7.53 (m, m/e 396 2- 2H), 7.47-7.28 (m, 1H), 4.94-4.67 (m, 4H), (M + H)⁺ yl]carbamoyl}phenyl)- 4.61-4.34 (m, 1H), 3.08-2.71 (m, 1H), 1.93-1.49 (m, 5,7-dihydro-6H- 2H), 1.00-0.70 (m, 6H) pyrrolo[3,4-b]pyridine- 6-carboxamide 1134 N-{4-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) cyclohexylpiperazin-1- 8.48 (d, J = 4.6 Hz, 1H), 7.91-7.76 (m, 1H), m/e 434 yl)carbonyl]phenyl}- 7.75-7.57 (m, 2H), 7.50-7.27 (m, 3H), 4.86 (t, J = 26.6 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 3.80 (s, 3H), 3.28-3.13 (m, 2H), 3.05-2.73 (m, pyrrolo[3,4-b]pyridine- 3H), 2.70-2.43 (m, 1H), 2.09 (d, J = 11.0 Hz, 2H), 6-carboxamide 1.84 (t, J = 13.9 Hz, 2H), 1.64 (d, J = 12.9 Hz, 1H), 1.48-1.22 (m, 4H), 1.22-1.04 (m, 1H) 1135 N-{4-[(3-tert- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) butoxypropyl)carbamoyl]phenyl}- 8.48 (d, J = 4.4 Hz, 1H), 7.80 (t, J = 17.2 Hz, 1H), m/e 394 5,7- 7.76-7.65 (m, 2H), 7.68-7.52 (m, 2H), 7.36 (dd, J = 7.7, (M + H)⁺ dihydro-6H- 5.0 Hz, 1H), 4.82 (d, J = 9.6 Hz, 4H), 3.48-3.33 (m, pyrrolo[3,4-b]pyridine- 3H), 1.73 (p, J = 6.5 Hz, 2H), 1.15 (s, 9H) 6-carboxamide 1136 N-(4-{[2-(2,6- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dimethylmorpholin-4- 8.47 (d, J = 5.0 Hz, 1H), 7.89-7.72 (m, 3H), m/e 424 yl)ethyl]carbamoyl}phenyl)- 7.70-7.53 (m, 2H), 7.48-7.18 (m, 1H), 4.87 (dd, J = 42.6, 12.8 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 3.97-3.75 (m, 2H), 3.75-3.58 (m, 2H), pyrrolo[3,4-b]pyridine- 3.53 (d, J = 12.0 Hz, 2H), 3.00-2.80 (m, 1H), 2.73 (t, 6-carboxamide J = 11.7 Hz, 2H), 2.51 (dt, J = 3.7, 1.8 Hz, 2H), 1.18 (d, J = 6.3 Hz, 6H) 1137 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxybenzyl)carbamoyl]phenyl}- 8.52-8.30 (m, 1H), 7.89-7.70 (m, 3H), 7.70-7.48 (m, m/e 403 5,7- 2H), 7.34 (dd, J = 7.7, 5.0 Hz, 1H), 7.23 (t, J = 8.0 Hz, (M + H)⁺ dihydro-6H- 1H), 6.99-6.84 (m, 2H), 6.86-6.69 (m, 1H), 4.82 (d, pyrrolo[3,4-b]pyridine- J = 10.4 Hz, 4H), 4.45 (s, 2H), 3.75 (s, 3H), 1.96 (s, 6-carboxamide 1H) 1138 N-(4-{[2-methyl-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.45 (t, (ESI(+)) (morpholin-4- J = 21.3 Hz, 1H), 7.89-7.74 (m, 3H), 7.80-7.58 (m, m/e 424 yl)propyl]carbamoyl}phenyl)- 2H), 7.34 (dd, J = 7.7, 5.0 Hz, 1H), 4.82 (d, J = 11.1 Hz, (M + H)⁺ 5,7-dihydro- 4H), 3.92 (s, 4H), 3.64 (s, 2H), 3.39 (s, 3H), 6H-pyrrolo[3,4- 1.39 (s, 6H) b]pyridine-6- carboxamide 1139 N-(4-{[(3S)-1-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 2-oxoazepan-3- 8.64-8.35 (m, 1H), 7.87-7.78 (m, 1H), 7.78-7.71 (m, m/e 408 yl]carbamoyl}phenyl)- 1H), 7.71-7.59 (m, 2H), 7.47-7.28 (m, 1H), (M + H)⁺ 5,7-dihydro-6H- 4.99-4.68 (m, 4H), 3.74-3.58 (m, 1H), 3.06-2.86 (m, pyrrolo[3,4-b]pyridine- 3H), 2.90-2.71 (m, 1H), 2.03-1.74 (m, 4H), 6-carboxamide 1.59-1.28 (m, 2H) 1140 N-(4-{[2-(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpiperazin-1- 8.48 (d, J = 4.4 Hz, 1H), 7.86-7.72 (m, 3H), m/e 409 yl)ethyl]carbamoyl}phenyl)- 7.72-7.58 (m, 2H), 7.35 (dd, J = 7.7, 5.0 Hz, 1H), 4.82 (d, J = 10.5 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 3.53 (t, J = 6.4 Hz, 2H), 3.32-3.22 (m, pyrrolo[3,4-b]pyridine- 4H), 3.20-3.02 (m, 4H), 2.97 (t, J = 6.4 Hz, 3H), 6-carboxamide 2.80 (s, 4H) 1141 N-(4-{[4-(morpholin- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 4- 8.60-8.40 (m, 1H), 7.93-7.71 (m, 3H), 7.73-7.49 (m, m/e 457 yl)benzyl]carbamoyl}phenyl)- 2H), 7.42-7.26 (m, 1H), 7.29-7.02 (m, 2H), (M + H)⁺ 5,7-dihydro- 6.98-6.81 (m, 2H), 4.81 (d, J = 11.8 Hz, 4H), 4.37 (d, J = 16.6 Hz, 6H-pyrrolo[3,4- 2H), 3.89-3.61 (m, 4H), 3.18-2.93 (m, b]pyridine-6- 4H), 2.98-2.74 (m, 1H) carboxamide 1142 N-(4-{[3-(piperidin-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) yl)propyl]carbamoyl}phenyl)- 8.47 (d, J = 4.2 Hz, 1H), 7.89-7.70 (m, 3H), m/e 408 5,7-dihydro- 7.73-7.51 (m, 2H), 7.33 (dd, J = 7.7, 5.0 Hz, 1H), 4.81 (d, J = 11.5 Hz, (M + H)⁺ 6H-pyrrolo[3,4- 4H), 3.38 (dd, J = 18.6, 12.0 Hz, 4H), b]pyridine-6- 3.21-3.00 (m, 2H), 2.92 (d, J = 19.7 Hz, 2H), 1.95 (tt, J = 33.3, carboxamide 15.0 Hz, 3H), 1.77 (d, J = 48.7 Hz, 6H) 1143 N-[4-(4,5,6,7- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) tetrahydro-1H-indazol- 8.45 (d, J = 7.5 Hz, 1H), 7.84-7.74 (m, 2H), 7.65 (dd, J = 18.3, m/e 403 5- 8.7 Hz, 2H), 7.56 (d, J = 8.7 Hz, 1H), (M + H)⁺ ylcarbamoyl)phenyl]- 7.41-7.19 (m, 2H), 4.90 (s, 1H), 4.81 (d, J = 14.4 Hz, 4H), 5,7-dihydro-6H- 2.87 (dd, J = 33.4, 22.8 Hz, 6H) pyrrolo[3,4-b]pyridine- 6-carboxamide 1195 N-{4-[(3-methoxy-2,2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.47 (t, (ESI(+)) dimethylpropyl)carbamoyl]phenyl}- J = 12.9 Hz, 1H), 7.85 (d, J = 7.7 Hz, 1H), m/e 388 5,7- 7.79-7.69 (m, 2H), 7.69-7.57 (m, 2H), 7.38 (dd, J = 7.7, 5.0 Hz, (M + H)⁺ dihydro-6H- 1H), 4.83 (d, J = 8.0 Hz, 4H), 3.30 (s, 3H), 3.21 (s, pyrrolo[3,4-b]pyridine- 2H), 3.15 (s, 2H), 0.90 (s, 6H) 6-carboxamide 1196 N-{4-[(3,3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dimethylbutyl)carbamoyl]phenyl}- 8.48 (d, J = 4.4 Hz, 1H), 7.82 (d, J = 7.7 Hz, 1H), m/e 367 5,7- 7.78-7.69 (m, 2H), 7.69-7.57 (m, 2H), 7.35 (dd, J = 7.7, (M + H)⁺ dihydro-6H- 5.0 Hz, 1H), 4.82 (d, J = 10.1 Hz, 4H), 3.31 (d, J = 4.0 Hz, pyrrolo[3,4-b]pyridine- 1H), 3.28 (s, 1H), 1.60-1.24 (m, 2H), 0.94 (s, 6-carboxamide 9H) 1197 N-(4-{[1-(furan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) yl)propan-2- 8.63-8.39 (m, 1H), 7.89-7.79 (m, 1H), 7.79-7.67 (m, m/e 391 yl]carbamoyl}phenyl)- 2H), 7.67-7.51 (m, 2H), 7.51-7.27 (m, 1H), (M + H)⁺ 5,7-dihydro-6H- 6.32 (dd, J = 3.1, 1.9 Hz, 1H), 6.13 (dd, J = 3.2, 0.7 Hz, pyrrolo[3,4-b]pyridine- 1H), 4.86 (t, J = 25.1 Hz, 4H), 4.28 (h, J = 6.7 Hz, 6-carboxamide 1H), 3.06-2.73 (m, 4H), 1.96 (s, 1H), 1.19 (t, J = 5.9 Hz, 3H) 1198 N-(4-{[(3-methyl-1,2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) oxazol-5- 8.59-8.37 (m, 1H), 7.87-7.70 (m, 3H), 7.71-7.52 (m, m/e 378 yl)methyl]carbamoyl}phenyl)- 2H), 7.42-7.20 (m, 1H), 6.24-6.02 (m, 1H), (M + H)⁺ 5,7-dihydro- 4.93-4.69 (m, 4H), 4.64-4.44 (m, 2H), 2.20 (s, 3H) 6H-pyrrolo[3,4- b]pyridine-6- carboxamide 1199 N-(4-{[(2R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.49 (t, (ESI(+)) cyanobutan-2- J = 7.9 Hz, 1H), 7.96-7.83 (m, 1H), 7.83-7.73 (m, m/e 364 yl]carbamoyl}phenyl)- 2H), 7.71-7.54 (m, 2H), 7.39 (dd, J = 7.7, 5.1 Hz, (M + H)⁺ 5,7-dihydro-6H- 1H), 4.83 (d, J = 7.3 Hz, 4H), 4.27-3.97 (m, 1H), pyrrolo[3,4-b]pyridine- 2.89-2.62 (m, 3H), 1.97 (s, 1H), 1.68 (p, J = 7.3 Hz, 6-carboxamide 2H), 0.93 (t, J = 7.4 Hz, 3H) 1200 N-{4-[methyl(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylbutyl)carbamoyl]phenyl}- 8.48 (dd, J = 5.4, 4.9 Hz, 1H), 7.84 (dd, J = 7.7, 0.7 Hz, m/e 367 5,7-dihydro- 1H), 7.72-7.50 (m, 2H), 7.47-7.32 (m, 1H), (M + H)⁺ 6H-pyrrolo[3,4- 7.34-7.16 (m, 2H), 4.86 (t, J = 25.0 Hz, 4H), 3.37 (dd, J = 14.4, b]pyridine-6- 6.9 Hz, 2H), 2.97-2.84 (m, 4H), 1.97 (s, 2H), carboxamide 1.66-1.33 (m, 3H), 1.06-0.63 (m, 6H) 1201 N-(4-{[(1-methyl-1H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyrazol-3- 8.47 (d, J = 4.9 Hz, 1H), 7.84-7.70 (m, 3H), m/e 377 yl)methyl]carbamoyl}phenyl)- 7.70-7.55 (m, 2H), 7.51 (t, J = 5.0 Hz, 1H), 7.32 (dd, J = 7.7, 4.9 Hz, (M + H)⁺ 5,7-dihydro- 1H), 6.15 (d, J = 2.2 Hz, 1H), 4.85 (t, J = 28.9 Hz, 6H-pyrrolo[3,4- 4H), 4.59-4.31 (m, 2H), 3.78 (d, J = 4.5 Hz, 3H) b]pyridine-6- carboxamide 1202 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxybutyl)carbamoyl]phenyl}- 8.49 (d, J = 4.9 Hz, 1H), 7.85 (t, J = 10.7 Hz, 1H), m/e 369 5,7- 7.78-7.69 (m, 2H), 7.68-7.49 (m, 2H), 7.43-7.30 (m, (M + H)⁺ dihydro-6H- 1H), 4.86 (t, J = 25.0 Hz, 4H), 3.35 (d, J = 4.6 Hz, pyrrolo[3,4-b]pyridine- 2H), 3.32 (d, J = 2.7 Hz, 3H), 1.71-1.34 (m, 2H), 6-carboxamide 0.90 (t, J = 7.4 Hz, 3H) 1203 N-(4-{[4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (dimethylamino)butyl]carbamoyl}phenyl)- 8.57-8.41 (m, 1H), 7.88-7.73 (m, 3H), 7.68-7.55 (m, m/e 382 5,7-dihydro-6H- 2H), 7.46-7.02 (m, 1H), 4.81 (d, J = 11.6 Hz, 4H), (M + H)⁺ pyrrolo[3,4-b]pyridine- 3.17-3.00 (m, 2H), 2.87-2.67 (m, 8H), 1.96 (s, 1H), 6-carboxamide 1.78-1.55 (m, 4H) 1204 N-(4-{[1-(1,3-thiazol- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.49 (t, (ESI(+)) 2- J = 5.3 Hz, 1H), 7.83 (d, J = 8.7 Hz, 3H), 7.67 (dt, J = 17.6, m/e 394 yl)ethyl]carbamoyl}phenyl)- 9.5 Hz, 3H), 7.61-7.47 (m, 1H), 7.34 (dt, J = 35.5, (M + H)⁺ 5,7-dihydro-6H- 17.8 Hz, 1H), 5.46 (q, J = 7.0 Hz, 1H), 4.83 (d, J = 9.3 Hz, pyrrolo[3,4-b]pyridine- 4H), 1.65 (d, J = 7.0 Hz, 3H) 6-carboxamide 1205 N-(4-{[1-(1-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 1H-pyrazol-4- 8.58-8.41 (m, 1H), 7.91-7.81 (m, 1H), 7.79-7.66 (m, m/e 391 yl)ethyl]carbamoyl}phenyl)- 2H), 7.70-7.58 (m, 2H), 7.58-7.51 (m, 1H), (M + H)⁺ 5,7-dihydro-6H- 7.37 (dd, J = 7.5, 5.2 Hz, 2H), 5.15 (q, J = 6.9 Hz, 1H), pyrrolo[3,4-b]pyridine- 4.82 (d, J = 8.4 Hz, 4H), 3.78 (s, 3H), 1.47 (t, J = 5.5 Hz, 6-carboxamide 3H) 1206 N-{4-[(3S)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.46 (t, (ESI(+)) tetrahydrofuran-3- J = 11.6 Hz, 1H), 7.87-7.70 (m, 3H), 7.70-7.52 (m, m/e 353 ylcarbamoyl]phenyl}- 2H), 7.35 (dt, J = 14.6, 7.3 Hz, 1H), 4.82 (d, J = 9.9 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 4.58-4.37 (m, 1H), 3.92-3.81 (m, 2H), pyrrolo[3,4-b]pyridine- 3.81-3.67 (m, 1H), 3.59 (dd, J = 8.9, 4.6 Hz, 1H), 6-carboxamide 2.31-2.11 (m, 1H), 2.02-1.76 (m, 2H) 1207 N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxybutan-2- 8.47 (dd, J = 15.1, 10.9 Hz, 1H), 7.84 (dd, J = 7.7, 1.0 Hz, m/e 369 yl)carbamoyl]phenyl}- 1H), 7.82-7.70 (m, 2H), 7.70-7.56 (m, 2H), (M + H)⁺ 5,7-dihydro-6H- 7.36 (dd, J = 7.7, 5.0 Hz, 1H), 4.82 (d, J = 9.1 Hz, 4H), pyrrolo[3,4-b]pyridine- 4.18-3.96 (m, 1H), 3.50-3.36 (m, 2H), 6-carboxamide 1.75-1.57 (m, 1H), 1.57-1.39 (m, 1H), 0.90 (t, J = 7.4 Hz, 3H) 1208 N-{4-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) aminobenzyl)carbamoyl]phenyl}- 8.47 (d, J = 4.2 Hz, 1H), 7.87-7.73 (m, 3H), m/e 388 5,7- 7.70-7.53 (m, 2H), 7.33 (dd, J = 8.0, 6.1 Hz, 3H), 7.09 (d, J = 8.3 Hz, (M + H)⁺ dihydro-6H- 2H), 4.81 (d, J = 11.4 Hz, 4H), 4.44 (s, 2H) pyrrolo[3,4-b]pyridine- 6-carboxamide 1209 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.47 (t, (ESI(+)) ethoxypropyl)carbamoyl]phenyl}- J = 11.3 Hz, 1H), 7.87-7.81 (m, 1H), 7.80-7.71 (m, m/e 369 5,7- 2H), 7.73-7.53 (m, 2H), 7.45-7.08 (m, 1H), 4.82 (d, (M + H)⁺ dihydro-6H- J = 9.2 Hz, 4H), 3.70-3.56 (m, 1H), 3.56-3.41 (m, pyrrolo[3,4-b]pyridine- 2H), 3.27 (dd, J = 13.4, 5.7 Hz, 1H), 1.18-0.88 (m, 6-carboxamide 6H) 1210 N-{4-[(6- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxypyridin-3- 8.58-8.32 (m, 2H), 8.10-7.96 (m, 1H), 7.96-7.85 (m, m/e 390 yl)carbamoyl]phenyl}- 2H), 7.85-7.74 (m, 1H), 7.74-7.60 (m, 2H), (M + H)⁺ 5,7-dihydro-6H- 7.40-7.14 (m, 1H), 6.97-6.64 (m, 1H), 5.01-4.62 (m, pyrrolo[3,4-b]pyridine- 4H), 3.87 (s, 3H) 6-carboxamide 1211 N-{4-[(2S)-butan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylcarbamoyl]phenyl}- 8.49 (d, J = 4.9 Hz, 1H), 7.83 (t, J = 12.3 Hz, 1H), m/e 339 5,7-dihydro-6H- 7.84-7.69 (m, 2H), 7.73-7.51 (m, 2H), 7.37 (dd, J = 7.7, (M + H)⁺ pyrrolo[3,4-b]pyridine- 5.0 Hz, 1H), 4.82 (d, J = 8.6 Hz, 4H), 3.92 (h, J = 6.7 Hz, 6-carboxamide 1H), 1.69-1.44 (m, 2H), 1.16 (d, J = 6.7 Hz, 3H), 0.89 (t, J = 7.4 Hz, 3H) 1212 N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) cyanocyclopropyl)carbamoyl]phenyl}- 8.47 (d, J = 4.7 Hz, 1H), 7.85-7.72 (m, 3H), m/e 348 5,7- 7.69-7.52 (m, 2H), 7.43-7.15 (m, 1H), 4.81 (d, J = 11.4 Hz, (M + H)⁺ dihydro-6H- 4H), 1.61-1.41 (m, 2H), 1.40-1.17 (m, 2H) pyrrolo[3,4-b]pyridine- 6-carboxamide 1213 N-(4-{[2-(5-methyl- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 1H-pyrazol-1- 8.55-8.36 (m, 1H), 7.87-7.75 (m, 1H), 7.75-7.67 (m, m/e 391 yl)ethyl]carbamoyl}phenyl)- 2H), 7.68-7.52 (m, 2H), 7.43-7.22 (m, 2H), (M + H)⁺ 5,7-dihydro-6H- 6.09-5.92 (m, 1H), 4.91-4.64 (m, 4H), 4.36-4.10 (m, pyrrolo[3,4-b]pyridine- 2H), 3.74-3.47 (m, 2H), 2.30-2.13 (m, 3H) 6-carboxamide 1214 N-(4-{[(4-methyl-1,3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) thiazol-2- 8.59-8.31 (m, 1H), 7.92-7.72 (m, 3H), 7.71-7.58 (m, m/e 394 yl)methyl]carbamoyl}phenyl)- 2H), 7.48-7.22 (m, 1H), 7.14-6.93 (m, 1H), 4.82 (d, (M + H)⁺ 5,7-dihydro- J = 11.0 Hz, 4H), 4.74-4.63 (m, 2H), 2.35 (d, J = 0.6 Hz, 6H-pyrrolo[3,4- 3H) b]pyridine-6- carboxamide 1215 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) hydroxypropyl)carbamoyl]phenyl}- 8.56-8.38 (m, 1H), 7.88-7.79 (m, 1H), 7.79-7.68 (m, m/e 341 5,7- 2H), 7.70-7.55 (m, 2H), 7.46-7.23 (m, 1H), 4.82 (d, (M + H)⁺ dihydro-6H- J = 9.5 Hz, 4H), 3.51 (t, J = 6.3 Hz, 2H), 3.3 (t, J = 6.3 Hz, pyrrolo[3,4-b]pyridine- 2H)1.83-1.60 (m, 2H) 6-carboxamide 1216 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpropyl)carbamoyl]phenyl}- 8.62-8.39 (m, 1H), 7.86-7.81 (m, 1H), 7.81-7.70 (m, m/e 339 5,7- 2H), 7.70-7.54 (m, 2H), 7.43-7.17 (m, 1H), (M + H)⁺ dihydro-6H- 4.84 (dd, J = 30.5, 23.8 Hz, 4H), 3.17-3.01 (m, 2H), pyrrolo[3,4-b]pyridine- 2.03-1.72 (m, 2H), 0.89 (t, J = 7.9 Hz, 6H) 6-carboxamide 1217 N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(tetrahydrofuran-2- 8.57-8.39 (m, 1H), 7.86-7.80 (m, 1H), 7.80-7.69 (m, m/e 367 ylmethyl)carbamoyl]phenyl}- 2H), 7.69-7.54 (m, 2H), 7.42-7.26 (m, 1H), 4.82 (d, (M + H)⁺ 5,7-dihydro- J = 10.1 Hz, 4H), 4.12-3.93 (m, 1H), 3.88-3.75 (m, 6H-pyrrolo[3,4- 1H), 3.74-3.54 (m, 1H), 3.33 (t, J = 5.9 Hz, 2H), b]pyridine-6- 1.98-1.78 (m, 4H), 1.71-1.51 (m, 1H) carboxamide 1218 N-(4-{[(1R)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.49 (t, (ESI(+)) cyclopropylethyl]carbamoyl}phenyl)- J = 5.8 Hz, 1H), 7.90-7.80 (m, 1H), 7.80-7.69 (m, m/e 351 5,7- 2H), 7.68-7.54 (m, 2H), 7.36 (dd, J = 7.7, 5.0 Hz, (M + H)⁺ dihydro-6H- 1H), 4.82 (d, J = 9.6 Hz, 4H), 3.64-3.41 (m, 1H), pyrrolo[3,4-b]pyridine- 1.23 (d, J = 6.7 Hz, 3H), 1.10-0.86 (m, 1H), 6-carboxamide 0.53-0.28 (m, 3H), 0.28-0.11 (m, 1H) 1219 N-(4-{[1-(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylcyclopropyl)ethyl]carbamoyl}phenyl)- 8.60-8.35 (m, 1H), 7.93-7.79 (m, 1H), 7.79-7.68 (m, m/e 365 5,7-dihydro-6H- 2H), 7.68-7.53 (m, 2H), 7.49-7.22 (m, 1H), 4.82 (d, (M + H)⁺ pyrrolo[3,4-b]pyridine- J = 9.2 Hz, 4H), 3.72 (q, J = 6.8 Hz, 1H), 1.17 (d, J = 6.8 Hz, 6-carboxamide 3H), 1.08 (s, 3H), 0.67-0.48 (m, 1H), 0.47-0.34 (m, 1H), 0.32-0.12 (m, 2H) 1220 N-{4-[(thiophen-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.45 (t, (ESI(+)) ylmethyl)carbamoyl]phenyl}- J = 8.3 Hz, 1H), 7.83-7.71 (m, 3H), 7.68-7.55 (m, m/e 379 5,7-dihydro- 2H), 7.39-7.21 (m, 1H), 7.08-6.98 (m, 1H), (M + H)⁺ 6H-pyrrolo[3,4- 6.99-6.90 (m, 1H), 4.80 (d, J = 12.9 Hz, 4H), 4.63 (s, 2H) b]pyridine-6- carboxamide 1221 N-(4-{[(1S)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) cyclopropylethyl]carbamoyl}phenyl)- 8.49 (d, J = 4.9 Hz, 1H), 7.85 (d, J = 7.7 Hz, 1H), m/e 350 5,7- 7.78-7.69 (m, 2H), 7.72-7.54 (m, 2H), 7.37 (dd, J = 7.7, (M + H)⁺ dihydro-6H- 5.0 Hz, 1H), 4.96-4.68 (m, 4H), 3.70-3.42 (m, 1H), pyrrolo[3,4-b]pyridine- 1.23 (d, J = 6.7 Hz, 3H), 1.15-0.90 (m, 1H), 6-carboxamide 0.58-0.16 (m, 4H) 1222 N-{4-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxybutyl)carbamoyl]phenyl}- 8.60-8.35 (m, 1H), 7.90-7.79 (m, 1H), 7.79-7.70 (m, m/e 369 5,7- 2H), 7.69-7.52 (m, 2H), 7.43-7.29 (m, 1H), 4.86 (t, (M + H)⁺ dihydro-6H- J = 24.4 Hz, 4H), 3.31-3.25 (m, 2H), 2.68-2.34 (m, pyrrolo[3,4-b]pyridine- 2H), 1.65-1.48 (m, 4H) 6-carboxamide 1223 N-(4-{[2-(tetrahydro- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 2H-pyran-3- 8.55-8.37 (m, 1H), 7.89-7.78 (m, 1H), 7.78-7.68 (m, m/e 395 yl)ethyl]carbamoyl}phenyl)- 2H), 7.68-7.52 (m, 2H), 7.43-7.02 (m, 1H), 4.86 (t, (M + H)⁺ 5,7-dihydro-6H- J = 25.4 Hz, 4H), 3.96-3.57 (m, 2H), 3.12-2.98 (m, pyrrolo[3,4-b]pyridine- 1H), 2.95-2.78 (m, 2H), 1.91-1.76 (m, 1H), 6-carboxamide 1.63-1.40 (m, 4H), 1.28-1.09 (m, 1H) 1224 N-(4-{[(2S)-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxypropan-2- 8.58-8.40 (m, 1H), 7.87-7.81 (m, 1H), 7.80-7.72 (m, m/e 355 yl]carbamoyl}phenyl)- 2H), 7.69-7.51 (m, 2H), 7.34 (dd, J = 7.7, 5.0 Hz, (M + H)⁺ 5,7-dihydro-6H- 1H), 4.81 (d, J = 11.0 Hz, 4H), 4.30-4.08 (m, 1H), pyrrolo[3,4-b]pyridine- 3.49-3.42 (m, 1H), 3.40-3.33 (m, 1H), 3.29 (s, 3H), 6-carboxamide 1.16 (t, J = 5.4 Hz, 3H) 1225 N-{4-[(3,3-dimethyl-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) oxobutyl)carbamoyl]phenyl}- 8.49 (d, J = 4.3 Hz, 1H), 7.89-7.81 (m, 1H), m/e 391 5,7-dihydro- 7.84-7.73 (m, 2H), 7.74-7.56 (m, 2H), 7.44-7.18 (m, 1H), (M + H)⁺ 6H-pyrrolo[3,4- 4.83 (d, J = 9.2 Hz, 4H), 4.30 (s, 2H), 1.18 (s, 9H) b]pyridine-6- carboxamide 1226 N-(4-{[(1-methyl-1H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyrrol-2- 8.58-8.35 (m, 1H), 7.92-7.71 (m, 3H), 7.70-7.49 (m, m/e 376 yl)methyl]carbamoyl}phenyl)- 2H), 7.44-7.19 (m, 1H), 4.82 (d, J = 9.5 Hz, 4H), (M + H)⁺ 5,7-dihydro- 4.44 (s, 2H), 3.59 (s, 3H) 6H-pyrrolo[3,4- b]pyridine-6- carboxamide 1227 N-(4-{[2-(propan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) yloxy)ethyl]carbamoyl}phenyl)- 8.60-8.37 (m, 1H), 7.86-7.72 (m, 3H), 7.71-7.56 (m, m/e 369 5,7-dihydro- 3H), 7.47-7.19 (m, 1H), 4.87-4.66 (m, 4H), (M + H)⁺ 6H-pyrrolo[3,4- 3.67-3.48 (m, 3H), 3.42-3.36 (m, 2H), 1.16-1.02 (m, 6H) b]pyridine-6- carboxamide 1228 N-(4-{[3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (dimethylamino)propyl]carbamoyl}phenyl)- 8.59-8.13 (m, 1H), 7.91-7.72 (m, 3H), 7.73-7.58 (m, m/e 368 5,7-dihydro-6H- 2H), 7.43-7.26 (m, 1H), 4.83 (t, J = 9.4 Hz, 4H), (M + H)⁺ pyrrolo[3,4-b]pyridine- 3.37 (d, J = 6.7 Hz, 2H), 3.27-3.07 (m, 2H), 2.81 (d, 6-carboxamide J = 4.7 Hz, 6H), 1.95 (d, J = 9.3 Hz, 2H) 1229 N-[4-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-3- 8.56-8.35 (m, 1H), 7.90-7.68 (m, 3H), 7.69-7.56 (m, m/e 367 ylcarbamoyl)phenyl]- 2H), 7.36 (td, J = 7.9, 4.0 Hz, 1H), 4.82 (d, J = 10.2 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 3.99-3.86 (m, 1H), 3.86-3.68 (m, 1H), pyrrolo[3,4-b]pyridine- 3.41-3.32 (m, 1H), 3.29-3.17 (m, 1H), 6-carboxamide 2.07-1.84 (m, 1H), 1.83-1.50 (m, 3H) 1230 N-(4-{[2-(1H-pyrrol-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) yl)ethyl]carbamoyl}phenyl)- 8.56-8.30 (m, 1H), 7.87-7.76 (m, 1H), 7.76-7.65 (m, m/e 376 5,7-dihydro-6H- 2H), 7.67-7.50 (m, 2H), 7.41-7.20 (m, 1H), 6.73 (t, (M + H)⁺ pyrrolo[3,4-b]pyridine- J = 2.0 Hz, 1H), 6.17-5.79 (m, 1H), 4.86-4.72 (m, 6-carboxamide 4H), 4.08 (t, J = 6.5 Hz, 2H), 3.57 (t, J = 6.5 Hz, 2H) 1231 N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxypropan-2- 8.49 (d, J = 4.8 Hz, 1H), 7.85 (t, J = 8.8 Hz, 1H), m/e 355 yl)carbamoyl]phenyl}- 7.81-7.70 (m, 2H), 7.70-7.52 (m, 2H), 7.51-7.22 (m, (M + H)⁺ 5,7-dihydro-6H- 1H), 4.82 (d, J = 9.0 Hz, 4H), 4.19 (h, J = 6.6 Hz, 1H), pyrrolo[3,4-b]pyridine- 3.59-3.43 (m, 1H), 3.30 (s, 3H), 2.88 (d, J = 50.6 Hz, 6-carboxamide 1H), 1.15 (dd, J = 10.7, 6.7 Hz, 3H) 1232 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) aminobenzyl)carbamoyl]phenyl}- 8.48 (d, J = 4.7 Hz, 1H), 7.92-7.76 (m, 3H), m/e 388 5,7- 7.74-7.51 (m, 2H), 7.32 (ddd, J = 15.4, 7.7, 4.6 Hz, 2H), (M + H)⁺ dihydro-6H- 7.18-7.08 (m, 2H), 7.00 (d, J = 7.9 Hz, 1H), 4.82 (d, J = 11.2 Hz, pyrrolo[3,4-b]pyridine- 4H), 4.47 (s, 2H) 6-carboxamide 1233 N-(4-{[(2R)-3- ¹H NMR (400 MHz, DMSO_D₂O) δ 8.56-8.39 (m, (ESI(+)) methylbutan-2- 1H), 7.92-7.80 (m, 1H), 7.80-7.68 (m, 2H), m/e 353 yl]carbamoyl}phenyl)- 7.68-7.53 (m, 2H), 7.53-6.97 (m, 1H), 4.83 (d, J = 7.2 Hz, (M + H)⁺ 5,7-dihydro-6H- 4H), 3.99-3.74 (m, 1H), 1.91-1.66 (m, 1H), 1.12 (d, pyrrolo[3,4-b]pyridine- J = 6.8 Hz, 3H), 0.99-0.82 (m, 6H) 6-carboxamide 1234 N-{4-[(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-3- 8.62-8.38 (m, 1H), 7.91-7.80 (m, 1H), 7.80-7.70 (m, m/e 381 ylmethyl)carbamoyl]phenyl}- 2H), 7.69-7.45 (m, 2H), 7.48-7.24 (m, 1H), 4.83 (d, (M + H)⁺ 5,7-dihydro- J = 8.0 Hz, 4H), 3.87-3.61 (m, 2H), 3.19-3.12 (m, 6H-pyrrolo[3,4- 3H), 1.92 (d, J = 34.0 Hz, 1H), 1.87-1.73 (m, 2H), b]pyridine-6- 1.67-1.55 (m, 1H), 1.55-1.37 (m, 1H), carboxamide 1.39-1.14 (m, 1H) 1235 N-{4-[(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpropyl)carbamoyl]phenyl}- 8.61-8.43 (m, 1H), 7.90-7.71 (m, 3H), 7.71-7.50 (m, m/e 355 5,7- 2H), 7.42-7.14 (m, 1H), 4.98-4.68 (m, 4H), (M + H)⁺ dihydro-6H- 3.04-2.66 (m, 2H), 1.29-1.01 (m, 6H) pyrrolo[3,4-b]pyridine- 6-carboxamide 1236 N-[4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (butylcarbamoyl)phenyl]- 8.55-8.42 (m, 1H), 7.85-7.77 (m, 1H), 7.79-7.68 (m, m/e 339 5,7-dihydro-6H- 2H), 7.68-7.54 (m, 2H), 7.47-6.86 (m, 1H), 4.80 (t, (M + H)⁺ pyrrolo[3,4-b]pyridine- J = 9.0 Hz, 4H), 3.26-3.17 (m, 2H), 1.63-1.49 (m, 6-carboxamide 2H), 1.46-1.27 (m, 2H), 0.92 (dd, J = 9.2, 5.5 Hz, 3H) 1237 N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [methyl(tetrahydrofuran- 8.57-8.37 (m, 1H), 7.90-7.72 (m, 1H), 7.66-7.52 (m, m/e 381 2- 2H), 7.45-7.34 (m, 1H), 7.33-7.16 (m, 2H), 4.86 (t, (M + H)⁺ ylmethyl)carbamoyl]phenyl}- J = 24.4 Hz, 4H), 4.21-3.97 (m, 1H), 3.86-3.55 (m, 5,7-dihydro- 2H), 3.57-3.39 (m, 2H), 3.08-2.97 (m, 3H), 6H-pyrrolo[3,4- 1.98-1.88 (m, 2H), 1.85-1.68 (m, 2H), 1.60-1.37 (m, 1H) b]pyridine-6- carboxamide 1238 N-{4-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ 8.49 (t, (ESI(+)) methoxyethyl)(methyl)carbamoyl]phenyl}- J = 5.2 Hz, 1H), 7.95-7.76 (m, 1H), 7.71-7.52 (m, m/e 355 5,7-dihydro-6H- 2H), 7.38-7.33 (m, 1H), 7.33-7.22 (m, 2H), 4.82 (d, (M + H)⁺ pyrrolo[3,4-b]pyridine- J = 9.0 Hz, 4H), 3.61-3.44 (m, 4H), 3.29-3.19 (m, 6-carboxamide 3H), 2.98 (s, 3H) 1239 N-{4-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) cyanoethyl)carbamoyl]phenyl}- 8.59-8.32 (m, 1H), 7.91-7.72 (m, 3H), 7.72-7.59 (m, m/e 336 5,7-dihydro- 2H), 7.40-7.20 (m, 1H), 5.03-4.86 (m, 1H), (M + H)⁺ 6H-pyrrolo[3,4- 4.88-4.68 (m, 4H), 1.72-1.43 (m, 3H) b]pyridine-6- carboxamide 1240 N-{4-[(3R)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) tetrahydrofuran-3- 8.48 (d, J = 4.4 Hz, 1H), 7.89-7.74 (m, 3H), m/e 353 ylcarbamoyl]phenyl}- 7.68-7.48 (m, 2H), 7.45-7.24 (m, 1H), 4.82 (d, J = 9.2 Hz, 4H), (M + H)⁺ 5,7-dihydro-6H- 4.59-4.28 (m, 1H), 3.94-3.83 (m, 2H), pyrrolo[3,4-b]pyridine- 3.80-3.64 (m, 1H), 3.65-3.51 (m, 1H), 2.37-2.00 (m, 1H), 6-carboxamide 2.05-1.80 (m, 1H) 1241 N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(cyclopentylmethyl)carbamoyl]phenyl}- 8.49 (d, J = 4.8 Hz, 1H), 7.90-7.80 (m, 1H), m/e 365 5,7- 7.80-7.68 (m, 2H), 7.68-7.49 (m, 2H), 7.47-7.11 (m, 1H), (M + H)⁺ dihydro-6H- 4.82 (d, J = 9.0 Hz, 4H), 3.26-3.10 (m, 2H), pyrrolo[3,4-b]pyridine- 2.36-2.07 (m, 1H), 1.75-1.45 (m, 6H), 1.39-1.18 (m, 2H) 6-carboxamide 1242 N-{4-[(2-methoxy-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpropyl)carbamoyl]phenyl}- 8.61-8.36 (m, 1H), 7.88-7.71 (m, 3H), 7.71-7.55 (m, m/e 369 5,7- 2H), 7.46-7.15 (m, 1H), 4.99-4.66 (m, 4H), 3.35 (d, (M + H)⁺ dihydro-6H- J = 4.5 Hz, 2H), 3.19-3.16 (m, 3H), 1.46-0.84 (m, pyrrolo[3,4-b]pyridine- 6H) 6-carboxamide 1243 N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(cyclopropylmethyl)carbamoyl]phenyl}- 8.60-8.40 (m, 1H), 7.85 (d, J = 7.7 Hz, 1H), 7.82-7.71 (m, m/e 337 5,7- 2H), 7.71-7.53 (m, 2H), 7.38 (dd, J = 7.7, 5.0 Hz, (M + H)⁺ dihydro-6H- 1H), 7.30-7.14 (m, 1H), 5.07-4.65 (m, 4H), 3.16 (t, pyrrolo[3,4-b]pyridine- J = 6.6 Hz, 2H), 1.20-0.87 (m, 1H), 0.52-0.37 (m, 6-carboxamide 2H), 0.32-0.06 (m, 2H) 1244 N-{4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [methyl(propyl)carbamoyl]phenyl}- 8.61-8.38 (m, 1H), 7.93-7.76 (m, 1H), 7.68-7.54 (m, m/e 339 5,7- 2H), 7.46-7.33 (m, 1H), 7.31-7.17 (m, 2H), (M + H)⁺ dihydro-6H- 4.97-4.59 (m, 4H), 2.92 (d, J = 8.0 Hz, 4H), 1.67-1.47 (m, pyrrolo[3,4-b]pyridine- 2H), 0.96-0.59 (m, 3H) 6-carboxamide 1245 N-{4-[(pyridin-4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylmethyl)carbamoyl]phenyl}- 8.83-8.62 (m, 2H), 8.52-8.39 (m, 1H), 7.96-7.77 (m, m/e 374 5,7-dihydro- 3H), 7.77-7.70 (m, 2H), 7.70-7.59 (m, 2H), (M + H)⁺ 6H-pyrrolo[3,4- 7.43-7.14 (m, 1H), 4.90-4.72 (m, 4H), 4.74-4.48 (m, 2H) b]pyridine-6- carboxamide

Example 293 N-{4-[(4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 293A N-(4-nitrophenyl)isoindoline-2-carboxamide

A solution of N-(4-aminophenyl)isoindoline-2-carboxamide (100 mg, 0.395 mmol), 4-phenylbutanoic acid (78 mg, 0.474 mmol), 1-hydroxybenzotriazole hydrate (66.5 mg, 0.434 mmol) and N-methylmorpholine (0.109 ml, 0.987 mmol) in N,N-dimethylformamide (1.771 ml) at room temperature was treated with N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (136 mg, 0.711 mmol). The mixture was stirred overnight and diluted with water (10 ml); the resulting suspension was filtered with water washes to give after drying product with an impurity. This solid was suspended in 2% methanol/dichloromethane and filtered to provide the title compound.

Example 293B N-(4-aminophenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 274, substituting N-(4-nitrophenyl)isoindoline-2-carboxamide for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 293C N-{4-[(4-phenylbutanoyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

A solution of N-(4-aminophenyl)isoindoline-2-carboxamide (100 mg, 0.395 mmol), 4-phenylbutanoic acid (78 mg, 0.474 mmol), 1-hydroxybenzotriazole hydrate (66.5 mg, 0.434 mmol) and N-methylmorpholine (0.109 ml, 0.987 mmol) in dimethylformamide (1.771 ml) at room temperature was treated with N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (136 mg, 0.711 mmol). The mixture was stirred overnight and diluted with water (10 ml); the resulting suspension was filtered with water washes to give product with an impurity. This solid was suspended in 2% methanol/methylene chloride and filtered to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 1.78-2.00 (m, 2H), 2.30 (t, J=7.3 Hz, 2H), 2.62 (t, J=7.5 Hz, 2H), 4.75 (s, 4H), 7.08-7.41 (m, 9H), 7.46 (s, 4H), 8.26 (s, 1H), 9.73 (s, 1H); (ESI(+)) m/e 400 (M+H)⁺.

TABLE 5 The following Examples were prepared essentially as described in Example 293, using an appropriate amine in Example 293A and substituting an appropriate carboxylic acid for 4-phenylbutanoic acid in Example 293C. Some products were purified by flash chromatography while others were purified by reverse-phase HPLC; accordingly, some Examples were isolated as trifluoroacetic acid salts. Ex Name ¹H NMR MS 291 N-{4-[(4,4,4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm (ESI(+)) trifluorobutanoyl)amino]phenyl}- 2.52-2.69 (m, 4H), 4.75 (s, 4H), 7.23-7.40 (m, 4H), m/e 378 1,3-dihydro-2H- 7.41-7.56 (m, 4H), 8.28 (s, 1H), 9.93 (s, 1H) (M + H)⁺ isoindole-2-carboxamide 292 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) ethoxypropanoyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.44 (s, 4H), m/e 354 1,3-dihydro-2H- 7.32-7.37 (m, 2H), 7.28-7.32 (m, 2H), 4.76 (s, 4H), (M + H)⁺ isoindole-2-carboxamide 3.68 (t, J = 6.3 Hz, 2H), 3.47 (q, J = 6.9 Hz, 2H), 2.50-2.55 (m, 2H), 1.11 (t, J = 6.9 Hz, 3H) 294 N-{4-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.90 (d, (ESI(+)) methylpentanoyl)amino]phenyl}- J = 6.4 Hz, 6 H), 1.40-1.63 (m, 3 H), m/e 352 1,3-dihydro-2H- 2.18-2.39 (m, 2 H), 4.75 (s, 4 H), 7.20-7.41 (m, 4 H,) (M + H)⁺ isoindole-2-carboxamide 7.45 (s, 4 H), 8.26 (s, 1 H), 9.72 (s, 1 H) 295 N-(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) {[(benzyloxy)acetyl]amino}phenyl)- Oxide, Temp = 90° C.) δ ppm 7.47 (s, 4H), m/e 402 1,3-dihydro-2H- 7.28-7.43 (m, 9H), 4.76 (s, 4H), 4.64 (s, 2H), 4.07 (s, (M + H)⁺ isoindole-2-carboxamide 2H) 296 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) m/e phenylpropanoyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.42 (s, 4H), 384 (M − H)⁻ 1,3-dihydro-2H- 7.22-7.37 (m, 8H), 7.15-7.20 (m, 1H), 4.76 (s, 4H), isoindole-2-carboxamide 2.93 (t, J = 7.6 Hz, 2H), 2.59-2.63 (m, 2H) 297 N-{4-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (APCI(+)) phenoxypropanoyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.45 (s, 4H), m/e 402 1,3-dihydro-2H- 7.26-7.36 (m, 6H), 6.92-6.96 (m, 2H), 6.91-6.95 (m, (M + H)⁺ isoindole-2-carboxamide 1H), 4.76 (s, 4H), 4.29 (t, J = 6.2 Hz, 2H), 2.76 (t, J = 6.2 Hz, 2H) 298 N-(4-{[N-(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) furoyl)glycyl]amino}phenyl)- Oxide, Temp = 90° C.) δ ppm 7.76 (dd, J = 1.8, 0.8 Hz, m/e 405 1,3-dihydro-2H-isoindole-2- 1H), 7.42-7.48 (m, 4H), 7.29-7.36 (m, 4H), (M + H)⁺ carboxamide 7.12 (dd, J = 3.5, 0.9 Hz, 1H), 6.62 (dd, J = 3.4, 1.7 Hz, 1H), 4.76 (s, 4H), 4.04 (s, 2H) 299 N-(4-{[4-(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (APCI(+)) thienyl)butanoyl]amino}phenyl)- Oxide, Temp = 90° C.) δ ppm 7.43 (s, 4H), m/e 406 1,3-dihydro-2H- 7.32-7.38 (m, 2H), 7.28-7.32 (m, 2H), 7.25 (dd, J = 5.2, (M + H)⁺ isoindole-2-carboxamide 1.2 Hz, 1H), 6.94 (dd, J = 5.0, 3.4 Hz, 1H), 6.86 (dq, J = 3.3, 1.1 Hz, 1H), 4.76 (s, 4H), 2.87 (ddd, J = 8.1, 7.1, 1.0 Hz, 2H), 2.37 (t, J = 7.3 Hz, 2H), 1.96 (p, J = 7.4 Hz, 2H) 300 N-{4-[(4-oxo-4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) m/e phenylbutanoyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.96-7.99 (m, 2H), 412 (M − H)⁻ 1,3-dihydro-2H-isoindole- 7.60-7.65 (m, 1H), 7.50-7.56 (m, 2H), 7.43 (s, 2-carboxamide 4H), 7.32-7.37 (m, 2H), 7.28-7.32 (m, 2H), 4.76 (s, 4H), 3.32 (t, J = 6.6 Hz, 2H), 2.72 (t, J = 6.6 Hz, 2H) 301 N-{4-[(N- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) benzoylglycyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.84-7.94 (m, 2H), m/e 415 1,3-dihydro-2H-isoindole- 7.52-7.57 (m, 1H), 7.48-7.51 (m, 2H), 7.46 (s, (M + H)⁺ 2-carboxamide 4H), 7.32-7.37 (m, 2H), 7.28-7.32 (m, 2H), 4.76 (s, 4H), 4.08 (s, 2H) 302 N-{4-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) m/e phenoxybutanoyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.44 (s, 4H), 414 (M − H)⁻ 1,3-dihydro-2H- 7.33-7.37 (m, 2H), 7.29-7.32 (m, 2H), 7.24-7.29 (m, isoindole-2-carboxamide 2H), 6.90-6.94 (m, 3H), 4.76 (s, 4H), 4.04 (t, J = 6.4 Hz, 2H), 2.47 (t, J = 7.3 Hz, 2H), 2.01-2.08 (m, 2H) 303 N-[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (propionylamino)phenyl]- Oxide, Temp = 90° C.) δ ppm 7.43 (s, 4H), m/e 310 1,3-dihydro-2H-isoindole-2- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 2.30 (q, J = 7.6 Hz, (M + H)⁺ carboxamide 2H), 1.11 (t, J = 7.5 Hz, 3H) 304 N-[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (pentanoylamino)phenyl]- Oxide, Temp = 90° C.) δ ppm 7.43 (s, 4H), m/e 338 1,3-dihydro-2H-isoindole-2- 7.32-7.37 (m, 2H), 7.28-7.32 (m, 2H), 4.76 (s, 4H), (M + H)⁺ carboxamide 2.28 (t, J = 7.4 Hz, 2H), 1.56-1.64 (m, 2H), 1.30-1.40 (m, 2H), 0.91 (t, J = 7.3 Hz, 3H) 305 N-[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (hexanoylamino)phenyl]-1,3- Oxide, Temp = 90° C.) δ ppm 7.43 (s, 4H), m/e 352 dihydro-2H-isoindole-2- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 2.27 (t, J = 7.4 Hz, (M + H)⁺ carboxamide 2H), 1.57-1.65 (m, 2H), 1.27-1.37 (m, 4H), 0.86-0.90 (m, 3H) 306 N-[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) (heptanoylamino)phenyl]- Oxide, Temp = 90° C.) δ ppm 7.43 (s, 4H), m/e 366 1,3-dihydro-2H-isoindole-2- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 2.28 (t, J = 7.4 Hz, (M + H)⁺ carboxamide 2H), 1.60 (p, J = 7.1 Hz, 2H), 1.25-1.39 (m, 6H), 0.83-0.91 (m, 3H) 307 N-[4-(pent-4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm (ESI(+)) enoylamino)phenyl]-1,3- 2.24-2.44 (m, 4H), 4.75 (s, 4H), 4.91-5.14 (m, 2H), m/e 336 dihydro-2H-isoindole-2- 5.72-5.97 (m, 1H), 7.25-7.40 (m, 4H), (M + H)⁺ carboxamide 7.46 (s, 4H), 8.26 (s, 1H), 9.76 (s, 1H) 308 N-{4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) [(ethoxyacetyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.47-7.50 (m, 4H), m/e 340 1,3-dihydro-2H-isoindole- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 3.99 (s, 2H), (M + H)⁺ 2-carboxamide 3.60 (q, J = 7.0 Hz, 2H), 1.21 (t, J = 6.9 Hz, 3H) 309 N-(4-{[(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) methoxyethoxy)acetyl]amino}phenyl)- Oxide, Temp = 90° C.) δ ppm 7.47 (s, 4H), m/e 370 1,3-dihydro-2H- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 4.04 (s, 2H), (M + H)⁺ isoindole-2-carboxamide 3.68-3.71 (m, 2H), 3.55-3.58 (m, 2H), 3.32 (s, 3H) 310 N-{4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) [(cyclopropylacetyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.44 (s, 4H), m/e 336 1,3-dihydro-2H- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 2.21 (d, J = 6.9 Hz, (M + H)⁺ isoindole-2-carboxamide 2H), 1.00-1.14 (m, 1H), 0.47-0.52 (m, 2H), 0.18-0.23 (m, 2H) 311 N-{4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(−)) m/e [(cyclopentylacetyl)amino]phenyl}- Oxide, Temp = 90° C.) δ ppm 7.43 (s, 4H), 362 (M − H)⁻ 1,3-dihydro-2H- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 2.25-2.30 (m, 3H), isoindole-2-carboxamide 1.73-1.81 (m, 2H), 1.49-1.64 (m, 4H), 1.18-1.27 (m, 2H) 312 N-(4-{[3-(4-methylpiperazin- ¹H NMR (400 MHz, DMSO-d₆/Deuterium (ESI(+)) 1- Oxide, Temp = 90° C.) δ ppm 7.42-7.48 (m, 4H), m/e 408 yl)propanoyl]amino}phenyl)- 7.29-7.36 (m, 4H), 4.76 (s, 4H), 3.22-3.25 (m, (M + H)⁺ 1,3-dihydro-2H-isoindole-2- 4H), 3.03 (t, J = 6.9 Hz, 2H), 2.97-3.01 (m, 4H), carboxamide 2.77 (s, 3H), 2.62 (t, J = 6.9 Hz, 2H) 564 5-cyano-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- 1H), 8.35 (s, 1H), 7.88 (s, 1H), 7.78 (dd, J = 7.9, m/e 389 1,3-dihydro-2H- 1.5 Hz, 1H), 7.58 (d, J = 7.9 Hz, 1H), (M + H)⁺ isoindole-2-carboxamide 7.51-7.40 (m, 4H), 4.84-4.76 (m, 4H), 2.31-2.15 (m, 3H), 1.81-1.67 (m, 2H), 1.67-1.45 (m, 4H), 1.29-1.11 (m, 2H) 596 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.68 (s, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- 1H), 8.23 (s, 1H), 7.50-7.38 (m, 4H), 7.25 (d, J = 8.4 Hz, m/e 394 5-methoxy-1,3- 1H), 6.95-6.91 (m, 1H), (M + H)⁺ dihydro-2H-isoindole-2- 6.90-6.83 (m, 1H), 4.68 (m, 4H), 3.76 (s, 3H), carboxamide 2.31-2.15 (m, 3H), 1.83-1.68 (m, 2H), 1.67-1.40 (m, 4H), 1.29-1.11 (m, 2H) 649 5-(hydroxymethyl)-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.80 (s, (ESI(+)) [(tetrahydrofuran-3- 1H), 8.28 (s, 1H), 7.46 (s, 4H), 7.33-7.28 (m, m/e 396 ylacetyl)amino]phenyl}-1,3- 2H), 7.27-7.21 (m, 1H), 5.21 (t, J = 5.6 Hz, (M + H)⁺ dihydro-2H-isoindole-2- 1H), 4.73 (bs, 4H), 4.51 (d, J = 5.6 Hz, 2H), carboxamide 3.85-3.70 (m, 2H), 3.64 (q, J = 7.6 Hz, 1H), 2.61-2.52 (m, 2H), 2.42-2.32 (m, 2H), 2.12-1.94 (m, 1H), 1.62-1.47 (m, 1H) 650 5-(hydroxymethyl)-N-(4- ¹H NMR (300 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) {[(2- ppm 9.19 (s, 1H), 8.05 (s, 1H), 7.48 (m, 4H), m/e 400 methoxyethoxy)acetyl]amino}phenyl)- 7.31-7.19 (m, 3H), 4.86 (bs, 1H), 4.74 (bs, 4H), (M + H)⁺ 1,3-dihydro-2H- 4.53 (bs, 2H), 4.04 (s, 2H), 3.74-3.66 (m, 2H), isoindole-2-carboxamide 3.60-3.52 (m, 2H), 3.32 (s, 3H) 682 5-(hydroxymethyl)-N-{4- ¹H NMR (300 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(tetrahydrofuran-2- ppm 9.41 (bs, 1H), 8.01 (bs, 1H), 7.45-7.41 (m, m/e 396 ylacetyl)amino]phenyl}-1,3- 4H), 7.30-7.22 (m, 3H), 4.87 (bs, 1H), 4.73 (bs, (M + H)⁺ dihydro-2H-isoindole-2- 4H), 4.52 (bs, 2H), 4.22-4.14 (m, 1H), carboxamide 3.82-3.75 (m, 1H), 3.66-3.59 (m, 1H), 2.53 (dd, J = 14.1, 7.0 Hz, 1H), 2.40 (dd, J = 14.0, 6.1 Hz, 1H), 2.05-1.94 (m, 1H), 1.92-1.76 (m, 2H), 1.64-1.51 (m, 1H) 683 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.52 (s, (ESI(+)) [(ethoxyacetyl)amino]phenyl}- 1H), 8.29 (s, 1H), 7.56-7.44 (m, 4H), m/e 370 5-(hydroxymethyl)-1,3- 7.33-7.20 (m, 3H), 5.20 (t, J = 5.6 Hz, 1H), 4.73 (bs, (M + H)⁺ dihydro-2H-isoindole-2- 4H), 4.51 (d, J = 5.6 Hz, 2H), 4.00 (s, 2H), carboxamide 3.56 (q, J = 7.0 Hz, 2H), 1.19 (t, J = 7.0 Hz, 3H) 684 5-(hydroxymethyl)-N-{4- ¹H NMR (300 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(tetrahydro-2H-pyran-4- ppm 9.43 (bs, 1H), 8.00 (bs, 1H), 7.44-7.41 (m, m/e 410 ylacetyl)amino]phenyl}-1,3- 4H), 7.30-7.20 (m, 3H), 4.87 (bs, 1H), 4.73 (bs, (M + H)⁺ dihydro-2H-isoindole-2- 4H), 4.52 (bs, 2H), 3.86-3.78 (m, 2H), carboxamide 3.38-3.26 (m, 2H), 2.23 (d, J = 7.0 Hz, 2H), 2.07-1.94 (m, 1H), 1.66-1.58 (m, 2H), 1.35-1.20 (m, 2H) 685 5-(hydroxymethyl)-N-{4- ¹H NMR (300 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(morpholin-4- ppm 9.32 (bs, 1H), 8.04 (bs, 1H), 7.49-7.45 (m, m/e 411 ylacetyl)amino]phenyl}-1,3- 4H), 7.32-7.22 (m, 3H), 4.89-4.83 (m, 1H), (M + H)⁺ dihydro-2H-isoindole-2- 4.74 (bs, 4H), 4.53 (bs, 2H), 3.68-3.62 (m, 4H), carboxamide 3.10 (s, 2H), 2.57-2.51 (m, 4H) 789 N-{4- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- Temp = 90° C.) δ ppm 7.39 (m, 4H), 7.16 (dd, J = 9.1, m/e 382 5-fluoro-1,3-dihydro- 2.6, 1H), 7.09 (m, 1H), 4.75 (bs, 2H), (M + H)⁺ 2H-isoindole-2-carboxamide 4.72 (bs, 2H), 2.27 (m, 4H), 1.76 (m, 2H), 1.57 (m, 4H), 1.24 (m, 2H) 791 N-{4- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- Temp = 90° C.) δ 7.70 (s, 1H), 7.64 (dd, J = 8.0, m/e 432 5-(trifluoromethyl)- 1.6, 1H), 7.58 (d, J = 8.0, 1H), 7.48-7.41 (m, (M + H)⁺ 1,3-dihydro-2H-isoindole-2- 3H), 4.83 (s, 3H), 2.32-2.25 (m, 3H), carboxamide 1.81-1.71 (m, 2H), 1.66-1.47 (m, 4H), 1.28-1.16 (m, 2H) 792 4-cyano-N-{4- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- Temp = 90° C.) δ 7.70 (ddd, J = 12.2, 7.7, 0.8, 2H), m/e 389 1,3-dihydro-2H- 7.52 (d, J = 7.7, 1H), 7.45 (m, 5H), 4.93 (d, J = 1.3, (M + H)⁺ isoindole-2-carboxamide 2H), 4.83 (d, J = 0.7, 2H), 2.28 (m, 4H), 1.77 (m, 2H), 1.57 (m, 4H) 793 N-{4- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- Temp = 90° C.) δ 7.42 (s, 4H), 7.22 (d, J = 7.8, m/e 378 5-methyl-1,3-dihydro- 1H), 7.15 (s, 1H), 7.15-7.08 (m, 1H), 4.70 (bs, (M + H)⁺ 2H-isoindole-2-carboxamide 4H), 2.35-2.23 (m, 4H), 1.82-1.71 (m, 2H), 1.66-1.47 (m, 4H), 1.30-1.16 (m, 2H) 794 4-chloro-N-{4- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- Temp = 90° C.) δ 7.43 (m, 4H), 7.33 (m, 3H), m/e 398 1,3-dihydro-2H- 4.83 (m, 2H), 4.78 (m, 2H), 2.28 (m, 3H), 1.77 (m, (M + H)⁺ isoindole-2-carboxamide 2H), 1.57 (m, 4H), 1.22 (m, 2H) 796 5-chloro-N-{4- ¹H NMR (400 MHz, DMSO-d₆/D₂O, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- Temp = 90° C.) δ 7.35 (m, 7H), 4.74 (d, J = 6.7, m/e 398 1,3-dihydro-2H- 4H), 2.27 (m, 3H), 1.78 (m, 2H), 1.57 (m, 4H), (M + H)⁺ isoindole-2-carboxamide 1.21 (m, 2H) 874 5-acetyl-N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- 1H), 8.33 (s, 1H), 7.96-7.88 (m, 2H), m/e 406 1,3-dihydro-2H- 7.54-7.40 (m, 5H), 4.81 (bs, 4H), 2.60 (s, 3H), (M + H)⁺ isoindole-2-carboxamide 2.31-2.18 (m, 3H), 1.81-1.68 (m, 2H), 1.68-1.43 (m, 4H), 1.25-1.10 (m, 2H) 878 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.68 (s, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- 1H), 8.25 (s, 1H), 7.47-7.44 (m, 4H), 7.32 (s, m/e 408 5-(1-hydroxyethyl)- 1H), 7.27 (s, 2H), 5.15 (d, J = 4.0 Hz, 1H), (M + H)⁺ 1,3-dihydro-2H-isoindole-2- 4.78-4.67 (m, 5H), 2.30-2.15 (m, 3H), carboxamide 1.82-1.68 (m, 2H), 1.67-1.45 (m, 4H), 1.33 (d, J = 6.4 Hz, 3H), 1.26-1.13 (m, 2H) 879 N-[4-(butyrylamino)phenyl]- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.72 (s, (ESI(+)) 5-cyano-1,3-dihydro-2H- 1H), 8.34 (s, 1H), 7.86 (s, 1H), 7.79-7.73 (m, m/e 349 isoindole-2-carboxamide 1H), 7.59-7.53 (d, J = 7.9 Hz, 1H), (M + H)⁺ 7.48-7.40 (m, 4H), 4.83-4.75 (m, 4H), 2.24 (t, J = 7.3 Hz, 2H), 1.65-1.53 (m, 2H), 0.90 (t, J = 7.4 Hz, 3H) 919 5-(acetamidomethyl)-N-{4- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- ppm 9.36 (bs, 1H), 8.04-7.95 (m, 2H), m/e 435 1,3-dihydro-2H- 7.48-7.39 (m, 4H), 7.30-7.17 (m, 3H), 4.73 (bs, 4H), (M + H)⁺ isoindole-2-carboxamide 4.27 (d, J = 5.9 Hz, 2H), 2.33-2.21 (m, 3H), 1.88 (s, 3H), 1.83-1.71 (m, 2H), 1.69-1.47 (m, 4H), 1.29-1.17 (m, 2H) 932 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- 1H), 8.25 (s, 1H), 7.50-7.41 (m, 5H), m/e 422 5-(2-hydroxypropan-2- 7.42-7.36 (m, 1H), 7.29-7.23 (m, 1H), 5.03 (s, 1H), (M + H)⁺ yl)-1,3-dihydro-2H- 4.72 (bs, 4H), 2.31-2.16 (m, 3H), isoindole-2-carboxamide 1.85-1.68 (m, 2H), 1.68-1.46 (m, 4H), 1.43 (s, 6H), 1.26-1.09 (m, 2H) 935 N-{4- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.69 (s, (ESI(+)) [(cyclopentylacetyl)amino]phenyl}- 1H), 8.27 (s, 1H), 7.51-7.40 (m, 4H), m/e 408 5-(methoxymethyl)- 7.36-7.22 (m, 3H), 4.74 (bs, 4H), 4.42 (s, 2H), 3.29 (s, (M + H)⁺ 1,3-dihydro-2H-isoindole-2- 3H), 2.35-2.15 (m, 3H), 1.81-1.68 (m, 2H), carboxamide 1.68-1.43 (m, 4H), 1.26-1.10 (m, 2H)

Example 313 methyl 2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate Example 313A methyl 2-(4-nitrophenylcarbamoyl)isoindoline-5-carboxylate

The title compound was prepared as described in Example 1A, substituting 4-nitrophenyl isocyanate for methyl 4-isocyanatobenzoate and methyl isoindoline-5-carboxylate hydrochloride for isoindoline.

Example 313B methyl 2-(4-aminophenylcarbamoyl)isoindoline-5-carboxylate

The title compound was prepared as described in Example 274, substituting methyl 2-(4-nitrophenylcarbamoyl)isoindoline-5-carboxylate for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 313C methyl 2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate

The title compound was prepared as described in Example 278, substituting methyl 2-(4-aminophenylcarbamoyl)isoindoline-5-carboxylate for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide and 2-cyclopentylacetyl chloride for acetyl chloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.69 (s, 1H), 8.32 (s, 1H), 7.94-7.94 (m, 1H), 7.89-7.96 (m, 1H), 7.51 (d, J=8.1 Hz, 1H), 7.41-7.49 (m, 4H), 4.75-4.82 (m, 4H), 3.87 (s, 3H), 2.24-2.29 (m, 2H), 2.15-2.28 (m, 1H), 1.68-1.81 (m, 2H), 1.44-1.67 (m, 4H), 1.13-1.24 (m, 2H); MS (ESI(+)) m/e 422 (M+H)⁺.

Example 314 2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic acid

The title compound was prepared as described in Example 1B, substituting methyl 2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylate for methyl 4-(isoindoline-2-carboxamido)benzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 12.97 (dd, J=4.1, 2.1 Hz, 1H), 9.70 (s, 1H), 8.32 (s, 1H), 7.88-7.92 (m, 2H), 7.46-7.50 (m, 1H), 7.43-7.48 (m, 4H), 4.79-4.81 (bs, 4H), 2.24-2.30 (m, 2H), 2.16-2.29 (m, 1H), 1.68-1.81 (m, 2H), 1.44-1.67 (m, 4H), 1.10-1.27 (m, 2H); MS (ESI(−)) m/e 406 (M−H)⁻.

Example 315 N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide

To a stirring suspension of 2-(4-(2-cyclopentylacetamido)phenylcarbamoyl)isoindoline-5-carboxylic acid (18 mg, 0.044 mmol) in tetrahydrofuran was added 1M borane in tetrahydrofuran (0.18 mL, 0.18 mml) dropwise. The mixture was heated at 60° C. for 1 hour. The reaction was cooled to room temperature and treated with several drops of 4M HCl-dioxane and methanol and then the clear solution was stirred at room temperature for 2 hours. The reaction was concentrated and purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.69 (s, 1H), 8.26 (s, 1H), 7.45 (s, 4H), 7.28-7.32 (m, 2H), 7.22-7.26 (m, 1H), 5.18-5.22 (m, 1H), 4.72-4.73 (bs, 4H), 4.50-4.53 (bs, 2H), 2.17-2.32 (m, 3H), 1.70-1.80 (m, 2H), 1.44-1.67 (m, 4H), 1.13-1.24 (m, 2H); MS (ESI(+)) m/e 394 (M+H)⁺.

Example 316 N-{4-[(2-cyclopentylethyl)amino]phenyl}-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide

To a stirring suspension of 2-(4-(2-cyclopentylacetamido)phenylcarbamoyl)isoindoline-5-carboxylic acid (18 mg, 0.044 mmol) in tetrahydrofuran was added 1M borane in tetrahydrofuran (0.18 mL, 0.18 mml) dropwise. The mixture was heated at 60° C. for 1 hour. The reaction was cooled to room temperature and treated with several drops of 4M HCl-dioxane and methanol and then the clear solution was stirred at room temperature for 2 hours. The reaction was concentrated and purified by reverse-phase HPLC to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.92 (s, 1H), 7.27-7.31 (m, 2H), 7.24 (d, J=8.1 Hz, 1H), 7.15-7.20 (m, 2H), 6.45-6.51 (m, 2H), 5.17-5.21 (m, 2H), 4.68-4.69 (bs, 4H), 4.51 (d, J=5.4 Hz, 2H), 2.97 (q, J=6.7 Hz, 2H), 1.70-1.95 (m, 3H), 1.42-1.66 (m, 6H), 1.04-1.20 (m, 2H); MS (ESI(+)) m/e 380 (M+H)⁺.

Example 317 tert-Butyl 4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate Example 317A N-(4-bromophenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 4-bromophenyl isocyanate for methyl 4-isocyanatobenzoate.

Example 317B tert-butyl 4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 280, substituting tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.38 (s, 1H), 7.55-7.57 (m, 2H), 7.26-7.42 (m, 6H), 6.06-6.09 (bs, 1H), 4.76-4.77 (bs, 4H), 3.97-4.00 (m, 2H), 3.51-3.55 (m, 2H), 2.42-2.46 (m, 2H), 1.43 (s, 9H); MS (ESI(−)) m/e 418 (M−H)⁻.

Example 318 N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.44 (s, 1H), 7.58-7.61 (m, 2H), 7.30-7.41 (m, 6H), 6.12-6.14 (bs, 1H), 4.77-4.78 (bs, 4H), 3.70-3.72 (m, 2H), 3.27-3.31 (m, 2H), 2.60-2.64 (m, 2H); MS (ESI(+)) m/e 320 (M+H)⁺.

Example 319 N-{4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-isopentyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.91 (d, J=6.4 Hz, 6H), 1.40-1.60 (m, 1H), 1.70 (q, J=6.8 Hz, 2H), 4.11 (t, J=7.1 Hz, 2H), 4.77 (s, 4H), 7.13-7.40 (m, 4H), 7.42-7.50 (m, 2H), 7.50-7.61 (m, 2H), 7.78 (s, 1H), 8.08 (s, 1H), 8.32 (s, 1H); MS (ESI(+)) m/e 375 (M+H)⁺.

Example 320 N-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 3.84 (s, 3H), 4.77 (s, 4H), 7.24-7.40 (m, 4H), 7.40-7.49 (m, 2H), 7.50-7.60 (m, 2H), 7.77 (s, 1H), 8.02 (s, 1H), 8.33 (s, 1H); MS (ESI(+)) m/e 319 (M+H)⁺.

Example 321 N-{4-[(1E)-5-phenylpent-1-en-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting (E)-4,4,5,5-tetramethyl-2-(5-phenylpent-1-enyl)-1,3,2-dioxaborolane for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 1.60-1.84 (m, 2H), 2.19 (q, J=7.0 Hz, 2H), 2.55-2.71 (m, 2H), 4.76 (s, 4H), 6.12-6.27 (m, 1H), 6.26-6.43 (m, 1H), 7.09-7.44 (m, 11H), 7.52 (d, J=8.5 Hz, 2H), 8.33 (s, 1H); MS (ESI(+)) m/e 383 (M+H)⁺.

Example 322 N-[4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-propyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.85 (t, J=7.3 Hz, 3H), 1.69-1.93 (m, 2H), 4.05 (t, J=6.9 Hz, 2H), 4.77 (s, 4H), 7.26-7.40 (m, 4H), 7.42-7.49 (m, 2H), 7.52-7.61 (m, 2H), 7.79 (s, 1H), 8.07 (s, 1H), 8.33 (s, 1H); MS (ESI(+)) m/e 347 (M+H)⁺.

Example 323 N-[4-(1-benzyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-benzyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 4.77 (s, 4H), 5.33 (s, 2H), 7.21-7.42 (m, 9H), 7.41-7.51 (m, 2H), 7.51-7.61 (m, 2H), 7.84 (s, 1H), 8.17 (s, 1H), 8.33 (s, 1H); MS (ESI(+)) m/e 395 (M+H)⁺.

Example 324 N-{4-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 2-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)ethanol for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 3.76 (q, J=5.8 Hz, 2H), 4.14 (t, J=5.6 Hz, 2H), 4.77 (s, 4H), 4.90 (t, J=5.4 Hz, 1H), 7.25-7.41 (m, 4H), 7.41-7.51 (m, 2H), 7.51-7.60 (m, 2H), 7.80 (s, 1H), 8.04 (s, 1H), 8.32 (s, 1H); MS (ESI(+)) m/e 349 (M+H)⁺.

Example 325 N-[6-(1-propyl-1H-pyrazol-4-yl)pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 325A N-(6-chloropyridin-3-yl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 2-chloro-5-isocyanatopyridine for methyl 4-isocyanatobenzoate.

Example 325B N-[6-(1-propyl-1H-pyrazol-4-yl)pyridin-3-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-propyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(6-chloropyridin-3-yl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.90-8.92 (bs, 1H), 8.84 (d, J=2.5 Hz, 1H), 8.39 (s, 1H), 8.25 (dd, J=8.8, 2.5 Hz, 1H), 8.08 (s, 1H), 7.87 (d, J=8.8 Hz, 1H), 7.31-7.41 (m, 4H), 4.79-4.83 (bs, 4H), 4.13 (t, J=6.9 Hz, 2H), 1.77-1.89 (m, 2H), 0.86 (t, J=7.3 Hz, 3H); MS (ESI(+)) m/e 348 (M+H)⁺.

Example 326 N-{6-[1-(3-methylbutyl)-1H-pyrazol-4-yl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-isopentyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(6-chloropyridin-3-yl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) 0.5 ppm 8.85-8.87 (bs, 1H), 8.81 (d, J=2.5 Hz, 1H), 8.38 (s, 1H), 8.21 (dd, J=8.8, 2.5 Hz, 1H), 8.05 (s, 1H), 7.82 (d, J=8.8 Hz, 1H), 7.31-7.41 (m, 4H), 4.78-4.83 (bs, 4H), 4.19 (t, J=7.1 Hz, 2H), 1.71 (q, J=7.0 Hz, 2H), 1.40-1.59 (m, 1H), 0.92 (d, J=6.6 Hz, 6H); MS (ESI(−)) m/e 374 (M−H)⁻.

Example 327 N-[4-(5-phenylpentyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 274, substituting N-{4-[(1E)-5-phenylpent-1-en-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) 0.5 ppm 1.21-1.40 (m, 4H), 1.49-1.67 (m, 4H), 2.45-2.62 (m, 2H), 4.75 (s, 4H), 7.05 (d, J=8.7 Hz, 2H), 7.14-7.40 (m, 9H), 7.44 (d, J=8.3 Hz, 2H), 8.23 (s, 1H); MS (ESI(+)) m/e 385 (M+H)⁺.

Example 328 N-[2-fluoro-4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 328A N-(4-bromo-2-fluorophenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 4-bromo-2-fluoro-1-isocyanatobenzene for methyl 4-isocyanatobenzoate.

Example 328B N-[2-fluoro-4-(1-propyl-1H-pyrazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-propyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromo-2-fluorophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) 0.5 ppm 8.19 (s, 1H), 8.03 (s, 1H), 7.89 (s, 1H), 7.57 (t, J=8.4 Hz, 1H), 7.46 (dd, J=12.1, 1.9 Hz, 1H), 7.24-7.39 (m, 5H), 4.76-4.78 (bs, 4H), 4.06 (t, J=6.9 Hz, 2H), 1.75-1.88 (m, 2H), 0.86 (t, J=7.3 Hz, 3H); MS (ESI(+)) m/e 365 (M+H)⁺.

Example 329 N-{2-fluoro-4-[1-(3-methylbutyl)-1H-pyrazol-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-isopentyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromo-2-fluorophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.21 (s, 1H), 8.04 (s, 1H), 7.88 (s, 1H), 7.56 (t, J=8.4 Hz, 1H), 7.46 (dd, J=12.1, 1.9 Hz, 1H), 7.25-7.41 (m, 5H), 4.76-4.81 (m, 4H), 4.12 (t, J=7.2 Hz, 2H), 1.70 (q, J=7.1 Hz, 2H), 1.40-1.59 (m, 1H), 0.91 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 330 N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting butyryl chloride for acetyl chloride and N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.38 (s, 1H), 7.55-7.58 (m, 2H), 7.27-7.38 (m, 6H), 6.09-6.11 (m, 1H), 4.77 (s, 4H), 4.08-4.14 (m, 2H), 3.58-3.68 (m, 2H), 2.39-2.51 (m, 2H), 2.34 (dt, J=19.8, 7.3 Hz, 2H), 1.46-1.62 (m, 2H), 0.88-0.93 (m, 3H); MS (ESI(+)) m/e 390 (M+H)⁺.

Example 331 N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting isobutyryl chloride for acetyl chloride and N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.40 (s, 1H), 7.55-7.58 (m, 2H), 7.30-7.38 (m, 6H), 6.11-6.13 (bs, 1H), 4.76-4.77 (bs, 4H), 4.19-4.21 (m, 1H), 4.08-4.09 (m, 1H), 3.65-3.72 (m, 2H), 2.85-3.00 (m, 1H), 2.40-2.56 (m, 2H), 1.00-1.07 (m, 6H); MS (ESI(+)) m/e 390 (M+H)⁺.

Example 332 N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.39 (s, 1H), 7.56-7.59 (m, 2H), 7.44-7.49 (m, 5H), 7.34-7.40 (m, 4H), 7.29-7.34 (m, 2H), 5.91-6.27 (m, 1H), 4.76-4.77 (bs, 4H), 4.02-4.26 (m, 2H), 3.36-3.59 (m, 2H), 2.51-2.61 (m, 2H); MS (ESI(+)) m/e 424 (M+H)⁺.

Example 333 N-{4-[1-(isopropylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 283, substituting propane-2-sulfonyl chloride for methanesulfonyl chloride and N-[4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.38-8.40 (m, 1H), 7.56-7.59 (m, 2H), 7.29-7.38 (m, 6H), 6.11-6.14 (m, 1H), 4.76-4.80 (m, 4H), 3.93-3.96 (m, 2H), 3.49 (t, J=5.5 Hz, 2H), 3.35-3.45 (m, 1H), 2.47-2.51 (m, 2H), 1.24 (d, J=6.9 Hz, 6H); MS (ESI(−)) m/e 424 (M−H)⁻.

Example 334 N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 334A tert-butyl 4-(5-(isoindoline-2-carboxamido)pyridin-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 280, substituting tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for 1H-pyrazol-3-ylboronic acid and N-(6-chloropyridin-3-yl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide.

Example 334B N-(6-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-3-yl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(5-(isoindoline-2-carboxamido)pyridin-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 334C tert-butyl 4-(5-(isoindoline-2-carboxamido)pyridin-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 278, substituting isobutyryl chloride for acetyl chloride and N-(6-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-3-yl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.70 (d, J=2.6 Hz, 1H), 8.33-8.37 (m, 1H), 7.95 (dd, J=8.6, 2.6 Hz, 1H), 7.44 (d, J=8.6 Hz, 1H), 7.28-7.36 (m, 4H), 6.54-6.56 (m, 1H), 4.79 (s, 4H), 4.16-4.18 (m, 2H), 3.68 (t, J=5.7 Hz, 2H), 2.86-2.97 (m, 1H), 2.54-2.63 (m, 2H), 1.04 (d, J=6.7 Hz, 6H); MS (ESI(−)) m/e 389 (M−H)⁻.

Example 335 N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(6-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-3-yl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.71 (d, J=2.5 Hz, 1H), 8.61 (s, 1H), 8.01 (dd, J=8.6, 2.2 Hz, 1H), 7.42-7.54 (m, 6H), 7.35-7.39 (m, 2H), 7.29-7.35 (m, 2H), 6.46-6.67 (m, 1H), 4.79 (s, 4H), 4.05-4.32 (m, 2H), 3.77-3.94 (m, 1H), 3.47-3.58 (m, 1H), 2.61-2.65 (m, 2H); MS (ESI(+)) m/e 425 (M+H)⁺.

Example 336 N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 336A N-(4-(piperazin-1-yl)phenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(isoindoline-2-carboxamido)phenyl)piperazine-1-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 336B N-[4-(4-benzoylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(4-(piperazin-1-yl)phenyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.14 (s, 1H), 7.38-7.50 (m, 7H), 7.28-7.38 (m, 4H), 6.87-6.91 (m, 2H), 4.74 (s, 4H), 3.39-3.90 (m, 4H), 3.01-3.17 (m, 4H); MS (ESI(+)) m/e 427 (M+H)⁺.

Example 337 N-{4-[4-(isopropylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 283, substituting isopropylsulfonyl chloride for methanesulfonyl chloride and N-(4-(piperazin-1-yl)phenyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.16 (s, 1H), 7.39-7.45 (m, 2H), 7.27-7.38 (m, 4H), 6.88-6.92 (m, 2H), 4.74 (s, 4H), 3.07-3.12 (m, 4H), 1.25 (d, J=6.8 Hz, 6H); MS (ESI(+)) m/e 429 (M+H)⁺.

Example 338 N-{4-[4-(phenylsulfonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 283, substituting benzenesulfonyl chloride for methanesulfonyl chloride and N-(4-(piperazin-1-yl)phenyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.14 (s, 1H), 7.65-7.80 (m, 5H), 7.35-7.41 (m, 2H), 7.27-7.37 (m, 4H), 6.81-6.85 (m, 2H), 4.72 (s, 4H), 3.09-3.15 (m, 4H), 2.99-3.04 (m, 4H); MS (ESI(−)) m/e 461 (M−H)⁻.

Example 339 N-{4-[3-(benzoylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 339A tert-butyl 1-(4-nitrophenyl)pyrrolidin-3-ylcarbamate

A solution of 1-fluoro-4-nitrobenzene (508 mg, 3.6 mmol) and tert-butyl pyrrolidin-3-ylcarbamate (671 mg, 3.6 mmol) in N,N-dimethylformamide (7 mL) was heated at 55° C. for 1.5 hours and then stirred overnight at room temperature. The reaction mixture was poured into water and the suspension was filtered with water washes to provide the title compound after drying.

Example 339B tert-butyl 1-(4-aminophenyl)pyrrolidin-3-ylcarbamate

The title compound was prepared as described in Example 274, substituting (+/−)-tert-butyl 1-(4-nitrophenyl)pyrrolidin-3-ylcarbamate for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 339C tert-butyl 1-(4-(isoindoline-2-carboxamido)phenyl)pyrrolidin-3-ylcarbamate

The title compound was prepared as described in Example 272, substituting (+/−)-tert-butyl 1-(4-aminophenyl)pyrrolidin-3-ylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride in Example 272B.

Example 339D N-[4-(3-aminopyrrolidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 2, substituting (+/−)-tert-butyl 1-(4-(isoindoline-2-carboxamido)phenyl)pyrrolidin-3-ylcarbamate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate in Example 2D.

Example 339E N-{4-[(3R)-3-(benzoylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide and N-{4-[(3S)-3-(benzoylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compounds were prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and (+/−)-N-(4-(3-aminopyrrolidin-1-yl)phenyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (d, J=6.8 Hz, 1H), 8.01 (s, 1H), 7.85-7.89 (m, 2H), 7.42-7.56 (m, 3H), 7.28-7.37 (m, 6H), 6.50 (d, J=8.7 Hz, 2H), 4.72 (s, 4H), 4.56-4.67 (m, 1H), 3.53-3.59 (m, 1H), 3.36-3.45 (m, 1H), 3.16-3.24 (m, 1H), 2.22-2.31 (m, 1H), 2.03-2.13 (m, 1H); MS (ESI(+)) m/e 427 (M+H)⁺.

Example 340 N-{4-[(3R)-3-(butyrylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide and N-{4-[(3S)-3-(butyrylamino)pyrrolidin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compounds were prepared as described in Example 278, substituting butyryl chloride for acetyl chloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.06 (d, J=6.9 Hz, 1H), 7.28-7.37 (m, 6H), 6.47 (d, J=8.7 Hz, 2H), 4.72 (s, 4H), 4.36 (h, J=5.7 Hz, 1H), 3.41-3.47 (m, 1H), 3.17-3.23 (m, 1H), 2.89-3.05 (m, 1H), 2.10-2.28 (m, 1H), 2.05 (t, J=7.3 Hz, 2H), 1.81-1.96 (m, 1H), 1.45-1.58 (m, 2H), 0.85 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 341 tert-butyl 4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperazine-1-carboxylate Example 341A tert-butyl 4-(4-nitrophenyl)piperazine-1-carboxylate

A solution of 1-fluoro-4-nitrobenzene (500 mg, 3.54 mmol) and tert-butyl piperazine-1-carboxylate (726 mg, 3.9 mmol) in dimethylformamide was treated with potassium carbonate (735 mg, 5.32 mmol) and the suspension was heated at 55° C. for 4 hours and then stirred overnight at room temperature. The reaction was poured into water and the suspension was filtered with water washes to provide the title compound after vacuum drying.

Example 341B tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate

The title compound was prepared as described in Example 274, substituting tert-butyl 4-(4-nitrophenyl)piperazine-1-carboxylate for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 341C tert-butyl 4-(4-(isoindoline-2-carboxamido)phenyl)piperazine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(4-aminophenyl)piperazine-1-carboxylate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.14 (s, 1H), 7.38-7.44 (m, 2H), 7.27-7.39 (m, 4H), 6.88-6.90 (m, 1H), 6.86 (s, 1H), 4.73 (s, 4H), 3.40-3.51 (m, 4H), 2.98-3.02 (m, 4H), 1.42 (s, 9H); MS (ESI(−)) m/e 421 (M−H)⁻.

Example 342 N-[4-(4-propionylpiperazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting propionyl chloride for acetyl chloride and N-(4-(piperazin-1-yl)phenyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.14 (s, 1H), 7.38-7.44 (m, 2H), 7.28-7.39 (m, 4H), 6.87-6.90 (m, 2H), 4.74 (s, 4H), 3.54-3.60 (m, 4H), 2.95-3.10 (m, 4H), 2.36 (q, J=7.4 Hz, 2H), 1.03 (s, 1H), 1.00 (d, J=7.4 Hz, 2H); MS (ESI(+)) m/e 379 (M+H)⁺.

Example 343 N-{4-[4-(cyclopropylcarbonyl)piperazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting cyclopropanecarbonyl chloride for acetyl chloride and N-(4-(piperazin-1-yl)phenyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.15 (s, 1H), 7.38-7.45 (m, 2H), 7.28-7.39 (m, 4H), 6.87-6.93 (m, 2H), 4.74 (s, 4H), 3.73-3.90 (m, 2H), 3.50-3.70 (m, 2H), 3.02-3.18 (m, 4H), 1.98-2.07 (m, 1H), 0.68-0.77 (m, 4H); MS (ESI(−)) m/e 389 (M−H)⁻.

Example 344 N-(2-butyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 344A tert-butyl 5-(isoindoline-2-carboxamido)isoindoline-2-carboxylate

In a 250 mL round bottom flask was mixed at room temperature triphosgene (234 mg, 0.790 mmol) in anhydrous dichloromethane (25 mL). To this solution was added dropwise over 15 minutes, a slurry of tert-butyl 5-aminoisoindoline-2-carboxylate (500 mg, 2.134 mmol) and diisopropylethylamine (0.410 ml, 2.347 mmol) in anhydrous dichloromethane (20 mL). The mixture was stirred overnight at room temperature. A solution of isoindoline (0.242 ml, 2.134 mmol) and diisopropylethylamine (0.410 ml, 2.347 mmol) in anhydrous dichloromethane (20 mL) was added in one portion. The reaction stirred overnight at room temperature. The solvent was removed and the residue was purified by normal phase flash chromatography to provide the title compound.

Example 344B N-(isoindolin-5-yl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 5-(isoindoline-2-carboxamido)isoindoline-2-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 344C N-(2-butyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting butyryl chloride for acetyl chloride and N-(isoindolin-5-yl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) 0.3 ppm 8.39 (s, 1H), 7.59-7.61 (bs, 1H), 7.43-7.48 (m, 1H), 7.30-7.41 (m, 4H), 7.22 (t, J=7.7 Hz, 1H), 4.77 (d, J=13.9 Hz, 2H), 4.77 (s, 4H), 4.55-4.60 (m, 2H), 2.33 (td, J=7.3, 3.7 Hz, 2H), 1.54-1.63 (m, 2H), 0.93 (td, J=7.3, 1.4 Hz, 3H); MS (ESI(+)) m/e 350 (M+H)⁺.

Example 345 N-(2-isobutyryl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting isobutyryl chloride for acetyl chloride and N-(isoindolin-5-yl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.40 (s, 1H), 7.59-7.61 (bs, 1H), 7.46 (ddd, J=10.8, 8.5, 2.1 Hz, 1H), 7.30-7.38 (m, 4H), 7.20-7.24 (m, 1H), 4.82-4.87 (m, 2H), 4.76-4.77 (bs, 4H), 4.55-4.60 (m, 2H), 2.78 (h, J=6.9 Hz, 1H), 1.07 (d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 350 (M+H)⁺.

Example 346 N-(2-benzoyl-2,3-dihydro-1H-isoindol-5-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(isoindolin-5-yl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.40 (d, J=8.8 Hz, 1H), 7.59-7.67 (m, 3H), 7.11-7.52 (m, 9H), 4.68-4.84 (m, 8H); MS (ESI(+)) m/e 384 (M+H)⁺.

Example 347 N-[2-(3-methylbutyl)-2,3-dihydro-1H-isoindol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 429, substituting 3-methylbutanal for isobutyraldehyde and N-(isoindolin-5-yl)isoindoline-2-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.28 (s, 1H), 7.47 (s, 1H), 7.29-7.37 (m, 5H), 7.09 (d, J=8.1 Hz, 1H), 4.75 (s, 4H), 3.77-3.79 (m, 2H), 3.74-3.76 (m, 2H), 2.64 (t, J=7.5 Hz, 2H), 1.60-1.71 (m, 1H), 1.37-1.43 (m, 2H), 0.91 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 350 (M+H)⁺.

Example 348 N-[4-(hexyloxy)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 1-(hexyloxy)-4-isocyanatobenzene for methyl 4-isocyanatobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.17 (s, 1H), 7.39-7.45 (m, 2H), 7.27-7.39 (m, 4H), 6.81-6.85 (m, 2H), 4.74 (s, 4H), 3.91 (t, J=6.5 Hz, 2H), 1.64-1.73 (m, 2H), 1.35-1.47 (m, 2H), 1.23-1.38 (m, 4H), 0.85-0.91 (m, 3H); MS (ESI(+)) m/e 339 (M+H)⁺.

Example 349 N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-[4-(piperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.39-7.47 (m, 3H) 7.22-7.40 (m, 6H) 6.27 (t, J=5.43 Hz, 1H) 4.56 (s, 4H) 4.36-4.52 (br s, 1H) 3.52 (br s, 1H) 3.00-3.15 (m, 2H) 2.93 (br s, 1H) 0.93-1.86 (series of br m, 12H); MS (ESI(+)) m/e 406 (M+H)⁺.

Example 350 N-{4-[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting nicotinoyl chloride hydrochloride for acetyl chloride and N-[4-(piperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58-8.71 (m, 2H) 7.87 (d, J=7.5 Hz, 1H) 7.52 (dd, J=7.5, 4.8 Hz, 1H) 7.22-7.36 (m, 4H) 6.28 (br m, 1H) 4.56 (s, 4H) 4.44 (br m, 1H) 3.38-3.57 (br m, 1H) 2.95-3.15 (br m, 2H) 2.68-2.84 (br m, 1H) 0.95-1.84 (br series of m, 12H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 351 N-[6-(4-chlorophenoxy)hexyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 344A, substituting 6-(4-chlorophenoxy)hexan-1-amine for tert-butyl 5-aminoisoindoline-2-carboxylate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 1.40 (q, 6H), 1.70 (q, 2H), 3.08 (q, J=6.8 Hz, 2H), 3.95 (t, J=6.4 Hz, 2H), 4.57 (s, 4H), 6.27 (t, J=5.4 Hz, 1H), 6.85-7.01 (m, 2H), 7.21-7.39 (m, 6H); MS (ESI(+)) m/e 373 (M+H)⁺.

Example 352 N-[4-(piperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 352A tert-butyl 4-(4-(isoindoline-2-carboxamido)butyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 344, substituting tert-butyl 4-(4-aminobutyl)piperidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate in Example 344A.

Example 352B N-[4-(piperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(isoindoline-2-carboxamido)butyl)piperidine-1-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 1.14-1.34 (m, 6H), 1.35-1.57 (m, 3H), 1.76 (d, J=12.30 Hz, 2H), 2.69-2.89 (m, 2H), 3.07 (q, J=6.74 Hz, 2H), 3.21 (d, J=12.70 Hz, 2H), 4.57 (s, 4H), 6.29 (t, J=5.55 Hz, 1H), 7.11-7.41 (m, 4H), 8.31 (s, 1H); MS (ESI(+)) m/e 299 (M+H)⁺.

Example 353 N,N′-hexane-1,6-diylbis(1,3-dihydro-2H-isoindole-2-carboxamide)

The title compound was prepared as described in Example 1A, substituting 1,6-diisocyanatohexane for methyl 4-isocyanatobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.19-7.37 (m, 8H) 6.28 (t, J=5.59 Hz, 2H) 4.57 (s, 8H) 3.07 (q, J=6.8 Hz, 4H) 1.37-1.55 (m, 4H) 1.21-1.37 (m, 4H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 354 N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting (4-isocyanatobutyl)benzene for methyl 4-isocyanatobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.24-7.33 (m, 6H), 7.13-7.22 (m, 3H), 6.30 (t, J=5.6 Hz, 1H), 4.56 (s, 4H), 3.06-3.13 (m, 2H), 2.59 (t, J=7.4 Hz, 2H), 1.51-1.65 (m, 2H), 1.40-1.53 (m, 2H); MS (ESI(+)) m/e 295 (M+H)⁺.

Example 355 ethyl 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoate

The title compound was prepared as described in Example 1A, substituting ethyl 6-isocyanatohexanoate for methyl 4-isocyanatobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.25-7.33 (m, 4H), 6.29 (t, J=5.6 Hz, 1H), 4.57 (s, 4H), 4.04 (q, J=7.1 Hz, 2H), 3.02-3.09 (m, 2H), 2.28 (t, J=7.3 Hz, 2H), 1.48-1.60 (m, 2H), 1.39-1.50 (m, 2H), 1.23-1.34 (m, 2H), 1.16 (t, J=7.1 Hz, 3H); MS (ESI(+)) m/e 305 (M+H)⁺.

Example 356 N-hexyl-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 1-isocyanatohexane for methyl 4-isocyanatobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.25-7.33 (m, 4H), 6.27 (t, J=5.6 Hz, 1H), 4.57 (s, 4H), 3.02-3.10 (m, 2H), 1.36-1.51 (m, 2H), 1.25-1.30 (m, 6H), 0.81-0.92 (m, 3H); MS (ESI(−)) m/e 245 (M−H)⁻.

Example 357 N-(3-phenylpropyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting (3-isocyanatopropyl)benzene for methyl 4-isocyanatobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.11-7.37 (m, 9H), 6.31 (t, J=5.5 Hz, 1H), 4.57 (s, 4H), 3.07-3.14 (m, 2H), 2.60 (t, J=7.6 Hz, 2H), 1.71-1.81 (m, 2H); MS (ESI(+)) m/e 281 (M+H)⁺.

Example 358 N-octyl-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 1-isocyanatooctane for methyl 4-isocyanatobenzoate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.24-7.35 (m, 4H), 6.27 (t, J=5.5 Hz, 1H), 4.57 (s, 4H), 3.02-3.09 (m, 2H), 1.40-1.47 (m, 2H), 1.25-1.27 (m, 10H), 0.81-0.89 (m, 3H); MS (ESI(+)) m/e 275 (M+H)⁺.

Example 359 N-{6-[(1-methyl-1H-pyrazol-4-yl)amino]-6-oxohexyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 359A 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoic acid

The title compound was prepared as described in Example 1B, substituting ethyl 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 359B N-{6-[(1-methyl-1H-pyrazol-4-yl)amino]-6-oxohexyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 1-methyl-1H-pyrazol-4-amine for 3-phenylpropan-1-amine and 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.81 (s, 1H), 7.82 (s, 1H), 7.34-7.36 (m, 1H), 7.24-7.34 (m, 4H), 6.28 (t, J=5.5 Hz, 1H), 4.56 (s, 4H), 3.75 (s, 3H), 3.03-3.10 (m, 2H), 2.22 (t, J=7.3 Hz, 2H), 1.51-1.64 (m, 2H), 1.40-1.52 (m, 2H), 1.23-1.34 (m, 2H); MS (ESI(+)) m/e 356 (M+H)⁺.

Example 360 N-[6-(methylamino)-6-oxohexyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting methylamine for 3-phenylpropan-1-amine and 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.60-7.72 (m, 1H), 7.25-7.33 (m, 4H), 6.24-6.29 (m, 1H), 4.57 (s, 4H), 2.94-3.09 (m, 2H), 2.54 (d, J=4.6 Hz, 3H), 2.30 (t, J=7.3 Hz, 1H), 2.04 (t, J=7.4 Hz, 1H), 1.37-1.58 (m, 4H), 1.18-1.35 (m, 2H); MS (ESI(+)) m/e 290 (M+H)⁺.

Example 361 N-{6-oxo-6-[(3-phenylpropyl)amino]hexyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.75-7.80 (m, 1H), 7.24-7.34 (m, 6H), 7.12-7.22 (m, 3H), 6.27 (t, J=5.5 Hz, 1H), 4.56 (s, 4H), 2.98-3.11 (m, 4H), 2.52-2.58 (m, 2H), 2.06 (t, J=7.3 Hz, 2H), 1.62-1.72 (m, 2H), 1.37-1.58 (m, 4H), 1.12-1.33 (m, 2H); MS (ESI(+)) m/e 394 (M+H)⁺.

Example 362 N-{6-[(3-methylbutyl)amino]-6-oxohexyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]hexanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.64-7.69 (m, 1H), 7.24-7.34 (m, 4H), 6.26 (t, J=5.5 Hz, 1H), 4.57 (s, 4H), 2.99-3.10 (m, 4H), 2.03 (t, J=7.3 Hz, 2H), 1.41-1.59 (m, 5H), 1.21-1.30 (m, 4H), 0.84 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 346 (M+H)⁺.

Example 363 N-{3-oxo-3-[(3-phenylpropyl)amino]propyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 363A ethyl 3-(isoindoline-2-carboxamido)propanoate

The title compound was prepared as described in Example 1A, substituting ethyl 3-isocyanatopropanoate for methyl 4-isocyanatobenzoate.

Example 363B 3-(isoindoline-2-carboxamido)propanoic acid

The title compound was prepared as described in Example 1B, substituting ethyl 3-(isoindoline-2-carboxamido)propanoate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 363C N-{3-oxo-3-[(3-phenylpropyl)amino]propyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-(isoindoline-2-carboxamido)propanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.87-7.92 (m, 1H), 7.22-7.32 (m, 6H), 7.12-7.19 (m, 3H), 6.36 (t, J=5.5 Hz, 1H), 4.56 (s, 4H), 3.24-3.32 (m, 2H), 3.03-3.10 (m, 2H), 2.52-2.60 (m, 2H), 2.30 (t, J=7.0 Hz, 2H), 1.63-1.74 (m, 2H); MS (ESI(+)) m/e 352 (M+H)⁺.

Example 364 N-{3-oxo-3-[4-(pyridin-2-yl)piperazin-1-yl]propyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 1-(pyridin-2-yl)piperazine for 3-phenylpropan-1-amine and 3-(isoindoline-2-carboxamido)propanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.11 (ddd, J=4.9, 2.0, 0.8 Hz, 1H), 7.53 (ddd, J=8.7, 7.0, 1.9 Hz, 1H), 7.25-7.34 (m, 4H), 6.83 (d, J=8.6 Hz, 1H), 6.65 (ddd, J=7.1, 4.9, 0.8 Hz, 1H), 6.37 (t, J=5.6 Hz, 1H), 4.57 (s, 4H), 3.44-3.61 (m, 8H), 3.28-3.37 (m, 2H), 2.54-2.61 (m, 2H); MS (ESI(+)) m/e 380 (M+H)⁺.

Example 365 N-{3-[(3-methylbutyl)amino]-3-oxopropyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 1 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 3-(isoindoline-2-carboxamido)propanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.76-7.81 (m, 1H), 7.25-7.34 (m, 4H), 6.31-6.36 (m, 1H), 4.56 (s, 4H), 3.23-3.31 (m, 2H), 3.02-3.09 (m, 2H), 2.27 (t, J=7.0 Hz, 2H), 1.46-1.62 (m, 1H), 1.27 (q, J=7.1 Hz, 2H), 0.84 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 304 (M+H)⁺.

Example 366 N-[4-(1-propyl-1H-pyrazol-4-yl)benzyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 366A N-(4-bromobenzyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 1-bromo-4-(isocyanatomethyl)benzene for methyl 4-isocyanatobenzoate.

Example 366B N-[4-(1-propyl-1H-pyrazol-4-yl)benzyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-propyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromobenzyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.85 (t, J=7.5 Hz, 3H), 1.70-1.92 (m, 2H), 4.06 (t, J=6.9 Hz, 2H), 4.29 (d, J=6.1 Hz, 2H), 4.63 (s, 4H), 6.91 (t, J=5.9 Hz, 1H), 7.18-7.40 (m, 6H), 7.49 (d, J=8.5 Hz, 2H), 7.82 (s, 1H), 8.12 (s, 1H); MS (ESI(+)) m/e 361 (M+H)⁺.

Example 367 N-[4-(1-isobutyl-1H-pyrazol-4-yl)benzyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-isobutyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and N-(4-bromobenzyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 0.86 (d, J=6.4 Hz, 6H), 2.03-2.21 (m, 1H), 3.91 (d, J=7.1 Hz, 2H), 4.28 (d, J=5.9 Hz, 2H), 4.63 (s, 4H), 6.92 (t, J=5.9 Hz, 1H), 7.25-7.37 (m, 6H), 7.50 (d, J=8.3 Hz, 2H), 7.83 (s, 1H), 8.10 (s, 1H); MS (ESI(+)) m/e 375 (M+H)⁺.

Example 368 N-(5-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(2-pyridyl)piperazine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)nicotinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.21 (s, 1H), 8.39 (dd, J=2.3, 0.8 Hz, 1H), 8.13 (dd, J=4.9, 1.9 Hz, 1H), 8.00 (dd, J=8.6, 0.8 Hz, 1H), 7.84 (dd, J=8.6, 2.4 Hz, 1H), 7.56 (ddd, J=8.7, 6.9, 1.9 Hz, 1H), 7.34-7.39 (m, 2H), 7.29-7.34 (m, 2H), 6.85 (d, J=8.5 Hz, 1H), 6.67 (dd, J=6.7, 4.9 Hz, 1H), 4.75-4.92 (bs, 4H), 3.47-3.81 (m, 8H); MS (ESI(+)) m/e 429 (M+H)⁺.

Example 369 N-{5-[(3-phenylpropyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 369A methyl 6-(isoindoline-2-carboxamido)nicotinate

The title compound was prepared as described in Example 344A, substituting methyl 6-aminonicotinate for tert-butyl 5-aminoisoindoline-2-carboxylate.

Example 369B 6-(isoindoline-2-carboxamido)nicotinic acid

The title compound was prepared as described in Example 1B, substituting methyl 6-(isoindoline-2-carboxamido)nicotinate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 369C N-{5-[(3-phenylpropyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 6-(isoindoline-2-carboxamido)nicotinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.25 (s, 1H), 8.74 (d, J=2.4 Hz, 1H), 8.47-8.51 (m, 1H), 8.14 (dd, J=8.8, 2.4 Hz, 1H), 8.00 (d, J=8.7 Hz, 1H), 7.33-7.38 (m, 2H), 7.29-7.33 (m, 2H), 7.26-7.30 (m, 2H), 7.21-7.26 (m, 2H), 7.15-7.21 (m, 1H), 4.74-4.92 (bs, 4H), 3.25-3.32 (m, 2H), 2.64 (t, J=7.6 Hz, 2H), 1.84 (p, J=7.4 Hz, 2H); MS (ESI(+)) m/e 401 (M+H)⁺.

Example 370 N-{5-[(3-methylbutyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)nicotinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.24 (s, 1H), 8.73 (d, J=2.4 Hz, 1H), 8.42 (t, J=5.5 Hz, 1H), 8.13 (dd, J=8.8, 2.4 Hz, 1H), 7.99 (d, J=8.7 Hz, 1H), 7.25-7.37 (m, 4H), 4.71-4.95 (bs, 4H), 3.24-3.32 (m, 2H), 1.57-1.68 (m, 1H), 1.43 (q, J=7.1 Hz, 2H), 0.91 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 353 (M+H)⁺.

Example 371 N-{5-[(3-phenylpropyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 371A methyl 2-(isoindoline-2-carboxamido)thiazole-5-carboxylate

The title compound was prepared as described in Example 272B, substituting methyl 2-aminothiazole-5-carboxylate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.

Example 371B 2-(isoindoline-2-carboxamido)thiazole-5-carboxylic acid

The title compound was prepared as described in Example 1B, substituting methyl 2-(isoindoline-2-carboxamido)thiazole-5-carboxylate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 371C N-{5-[(3-phenylpropyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 2-(isoindoline-2-carboxamido)thiazole-5-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 11.00-11.19 (bs, 1H), 8.34 (t, J=5.6 Hz, 1H), 7.98 (s, 1H), 7.15-7.37 (m, 9H), 4.70-4.83 (m, 4H), 3.17-3.28 (m, 2H), 2.63 (t, J=7.6 Hz, 2H), 1.81 (p, J=7.4 Hz, 2H); MS (ESI(−)) m/e 405 (M−H)⁻.

Example 372 N-{5-[(3-methylbutyl)carbamoyl]-1,3-thiazol-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 2-(isoindoline-2-carboxamido)thiazole-5-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 11.01-11.16 (bs, 1H), 8.27 (t, J=5.6 Hz, 1H), 7.96 (s, 1H), 7.29-7.36 (m, 4H), 4.73-4.88 (bs, 4H), 3.18-3.28 (m, 2H), 1.52-1.69 (m, 1H), 1.34-1.44 (m, 2H), 0.90 (d, J=6.6 Hz, 6H); MS (ESI(−)) m/e 357 (M−H)⁻.

Example 374 N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 374A N-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)isoindoline-2-carboxamide

500 mg (4-Isocyanatophenyl)boronic acid pinacolester (1.979 mmol) and 365 mg isoindoline (2.97 mmol) were dissolved in 10 ml dichloromethane and the resultant mixture was stirred over night at room temperature. After adding water, the mixture was extracted several times with dichloromethane, the combined organic phases were washed with dried over magnesium sulfate and filtered. The solvent was evaporated under reduced pressure. Column chromatography of the residue with dichloromethane resulted in the title compound.

Example 374B N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

105 mg N-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)isoindoline-2-carboxamide (0.288 mmol) and 53 mg 4-chloro-1,2-dihydrophthalazin-1-one (0.288 mmol) were dissolved in 2.5 ml dioxane. Cesium carbonate (474 mg, 1.44 mmol) was dissolved in 0.25 ml water and the resulting solution added to the reaction mixture. After the addition of 27.8 mg [1,1′-bis(diphenylphosphino)-ferrocene]dichlorpalladium(II) (0.038 mmol) the reaction mixture was flushed with nitrogen and stirred for 30 minutes in the microwave (Biotage Initiator 2.5) at 110° C. Dioxane was removed under reduced pressure, water and dichloromethane added to the residue and the formed precipitation was filtered. After dissolving the solid matter in a larger amount of dichloromethane/methanol 8:2, silica gel was added and subsequently the solvent was removed under reduced pressure. This residue was was purified by column chromatography using dichloromethane/methanol 95:5. ¹H NMR (DMSO-d₆, 400 MHz): 0.3 ppm 12.73 (s, 1H), 8.55 (s, 1H), 8.33 (dd, 1H), 7.85-7.92 (m, 2H), 7.73-7.78 (m, 3H), 7.48 (d, 2H), 7.35-7.38 (m, 2H), 7.30-7.33 (m, 2H), 4.81 (s, 4H). MS (ESI(−)) m/e 383.2 (M+H)⁺.

Example 375 N-[4-(isoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 374B, substituting 4-chloro-1,2-dihydrophthalazin-1-one with 4-bromoisoquinoline. ESI-MS [M+H+]=366.1.

Example 376 N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one. ESI-MS [M+H+]=382.1.

Example 377 N-[4-(4-oxo-3,4,5,6,7,8-hexahydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 377A 2-(4-Amino-benzoyl)-cyclohex-1-enecarboxylic acid

To a suspension of 2.2 g magnesium turnings (83.5 mmol) in 15 ml tetrahydrofuran were added 0.1 mL 1,2-dibromethane to start the Grignard reaction followed by slow addition of 13.0 g 2-(4-bromphenyl)-1,1,1,3,3,3-hexamethyldisilazane (41 mmol) in 70 mL tetrahydrofuran over a period of 20 minutes at room temperature with subsequent stirring for further 30 minutes. The resulting mixture was added dropwise at −78° C. to a solution of 4,5,6,7-tetrahydro-isobenzofuran-1,3-dione (5.6 g) in 70 mL tetrahydrofuran. The reaction mixture was slowly warmed to room temperature. Sulfuric acid (2 mL, 1 M) was added and the solvent was removed under reduced pressure. The residue was added carefully to 20 mL of 0.5 M sulfuric acid solution and the desired product started to precipitate and was extracted with ethyl acetate. Acidification of the water phase and extraction with ethyl acetate was continued until pH-4-5 (at least three times). The combined organic phases were washed with brine, dried over magnesium sulfate, filtered and the solvent was subsequently evaporated under reduced pressure. Purification of the raw material by column chromatography with ethyl acetate/hexane 1:1 and subsequently 100% ethyl acetate resulted in the desired product.

Example 377B 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one

10.3 g of 2-(4-amino-benzoyl)-cyclohex-1-enecarboxylic acid (42 mmol) were dissolved in 45 mL ethanol, 2.7 g (54 mmol) hydrazine hydrate was added and the mixture was heated under reflux for 30 hours. Precipitation of the product already started several hours after heating. After cooling in the refrigerator overnight the precipitated product was filtered and washed with cold ethanol.

Example 377C 1,3-dihydro-isoindole-2-carboxylicacid [4-(4-oxo-3,4,5,6,7,8-hexahydro-phthalazin-1-yl)-phenyl]-amide

To a solution of 200 mg 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one (0.829 mmol) in 5 ml N,N-dimethylformamide were added 245 mg carbonic acid bis-(2,5-dioxo-pyrrolidin-1-yl) ester (0.912 mmol) and the reaction mixture was stirred overnight. 255 mg of isoindoline were added, the precipitation formed was dissolved by adding 0.8 ml N,N-dimethylformamide, and the reaction mixture was stirred overnight. Water was added, and the formed precipitation was washed with water/methanol and subsequently dried in vacuum to obtain the crude material. The crude material was refluxed in 20 ml ethanol for 2 hours, cooled to room temperature, filtered and dried to obtain the desired product. ESI-MS [M+H+]=387.2.

Example 378 N-[4-(8-fluoro-4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-5-fluoro-2H-phthalazin-1-one. ESI-MS [M+H+]=401.1.

Example 379 5-fluoro-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with 5-fluoro-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=401.1.

Example 380 N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with 5-pyrrolidin-1-ylmethyl-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=466.2.

Example 381 5-(morpholin-4-ylmethyl)-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with 5-morpholin-4-ylmethyl-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=481.3.

Example 382 5-methoxy-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with 5-methoxy-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=412.2.

Example 383 5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with 5-(4-methyl-piperazin-1-ylmethyl)-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=495.2.

Example 384 5-cyano-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with 2,3-dihydro-1H-isoindole-5-carbonitrile. ESI-MS [M+H+]=407.1.

Example 385 5-chloro-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with 5-chloro-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=416.1.

Example 386 N-[4-(4-oxo-4,5-dihydro-3H-2,3-benzodiazepin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 1-(4-amino-phenyl)-3,5-dihydrobenzo[d][1,2]diazepin-4-one. ESI-MS [M+H+]=397.2.

Example 387 N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with 5-pyrrolidin-1-ylmethyl-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=465.2.

Example 388 N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-5-trifluoromethyl-2H-phthalazin-1-one. ESI-MS [M+H+]=451.1.

Example 389 5-[(dimethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with (2,3-dihydro-1H-isoindol-5-ylmethyl)-dimethyl-amine. ESI-MS [M+H+]=439.3.

Example 390 5-[(diethylamino)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with (2,3-dihydro-1H-isoindol-5-ylmethyl)-diethyl-amine. ESI-MS [M+H+]=467.3.

Example 391 5-[(4-methylpiperazin-1-yl)methyl]-N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-aminophenyl)isoquinolin-1(2H)-one and isoindoline with 5-(4-methyl-piperazin-1-ylmethyl)-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=494.3.

Example 392 5-[(dimethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with (2,3-dihydro-1H-isoindol-5-ylmethyl)-dimethyl-amine. ESI-MS [M+H+]=440.2.

Example 393 5-[(diethylamino)methyl]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with (2,3-dihydro-1H-isoindol-5-ylmethyl)-diethyl-amine. ESI-MS [M+H+]=468.2.

Example 394 N-{4-[4-oxo-8-(trifluoromethyl)-3,4-dihydrophthalazin-1-yl]phenyl}-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-5-trifluoromethyl-2H-phthalazin-1-one and isoindoline with 5-pyrrolidin-1-ylmethyl-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=534.2.

Example 395 5-[(1-methylpiperidin-4-yl)oxy]-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with 5-(1-methyl-piperidin-4-yloxy)-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=496.2.

Example 396 5-{[(3R)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with 5-((R)-3-fluoro-pyrrolidin-1-ylmethyl)-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=484.2.

Example 397 5-{[(3S)-3-fluoropyrrolidin-1-yl]methyl}-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with 54(S)-3-fluoro-pyrrolidin-1-ylmethyl)-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=484.2.

Example 398 5-(azetidin-1-ylmethyl)-N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2H-phthalazin-1-one and isoindoline with 5-azetidin-1-ylmethyl-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=452.2.

Example 399A N′-(4-bromobenzoyl)-1H-pyrrole-2-carbohydrazide

To 0.750 g of 1H-pyrrole-2-carbohydrazide (5.99 mmol) in 50 ml tetrahydrofuran was added 1.315 g 4-bromobenzoyl chloride (5.99 mmol) and 1 ml pyridine (11.99 mmol) at room temperature under nitrogen. After one hour of stirring at room temperature, the desired product precipitated. The precipitate was filtered, washed with minimum dichloromethane and methanol and dried to afford the title compound. ¹H NMR (400 MHz, DMSO-d₆) δ 11.63 (s, 1H), 10.47 (s, 1H), 10.04 (s, 1H), 7.84-7.88 (m, 2H), 7.75 (d, J=8.8, 1H), 7.75 (q, J=4.2, 1H), 6.91-6.95 (m, 2H), 6.33-6.15 (m, 1H).

Example 399B 2-(4-bromophenyl)-5-(1H-pyrrol-2-yl)-1,3,4-oxadiazole

To 1.2 g of N′-(4-bromobenzoyl)-1H-pyrrole-2-carbohydrazide (3.89 mmol) was added 5 ml phosphoryl trichloride (1.65 mmol). The reaction was stirred for 25 minutes at 120° C. The reaction was cooled to 0° C., and ice was added. The resulting solid was filtered, and washed with water, NH₄OH, dichloromethane and ethyl acetate. Purification by silica gel chromatography (dichloromethane:methanol=9:1) resulted in the desired product. ¹H NMR (400 MHz, DMSO-d₆) δ 12.32 (s, 1H), 8.05-8.00 (m, 2H), 7.89-7.83 (m, 2H), 7.18 (td, J=1.5, 2.6, 1H), 6.97 (ddd, J=1.5, 2.4, 3.7, 1H), 6.33 (dt, J=2.4, 3.6, 1H). ¹³C NMR (400 MHz, DMSO-d₆) δ 110.16, 112.49, 115.12, 122.71, 123.96, 125.23, 128.26, 132.49, 159.37, 161.57.

Example 399C 4-(4-bromophenyl)pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one

To 0.469 g sodium ethanolate (6.89 mmol) dissolved in 20 ml ethanol was added 1.0 g 2-(4-bromophenyl)-5-(1H-pyrrol-2-yl)-1,3,4-oxadiazole (3.45 mmol) at room temperature under nitrogen and the mixture was stirred at room temperature for 5 minutes. The reaction was heated at 160° C. for 2 hours in a microwave (Biotage Initiator 2.5). The reaction was monitored by TLC dichloromethane/methanol=9/1. Additional equivalents of sodium ethanolate were added and additional heating was carried out until completion of the reaction according to TLC. The reaction mixture was concentrated under reduced pressure and adsorbed on silica gel. The product was purified by silica gel chromatography (gradient: cyclohexane/ethylacetate=0-100%) to afford the title compound. ¹H NMR (400 MHz, DMSO-d₆) δ 12.09 (s, 1H), 7.85-7.78 (m, 2H), 7.76-7.69 (m, 2H), 7.39 (dd, J=1.3, 2.9, 1H), 7.16 (dd, J=1.4, 3.8, 1H), 6.77 (dd, J=2.9, 3.8, 1H). ¹³C NMR (400 MHz, DMSO-d₆) δ 154.22, 136.46, 131.98, 130.90, 129.52, 124.07, 124.00, 118.80, 114.42, 111.01.

Example 399D 4-(4-aminophenyl)pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one

To 1.181 g 4-(4-bromophenyl)pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one (4.07 mmol) in toluene (10 ml) was added 0.080 g 2-dicyclohexylphosphino-2′-(N,N-dimethylamino)biphenyl (0.2004 mmol), 0.063 g tris(dibenzylideneacetone)dipalladium(0) chloroform adduct (0.061 mmol) and 10.58 ml lithium bis(trimethylsilyl)amide 1M in toluene (10.58 mmol) under nitrogen at room temperature and the reaction was subsequently heated at 150° C. for 5 minutes by microwave (Biotage Initiator 2.5). Thin layer chromotography in cyclohexane/ethyl acetate=1/1 showed no starting material. After cooling the reaction mixture, 7 ml of 2N aqueous HCl was added, the mixture stirred for 30 minutes, and the mixture was basified until pH=10 by addition of aqueous NaOH (2N). A precipitate was formed. The solid was filtered and washed with ether and dried overnight to obtain the title compound. LCMS: m/z 227.0 (M+H). The filtrate was extracted with ethyl acetate. The organic phase was combined with the ether from the washing, dried over Na₂SO₄, filtered, and the solvent was evaporated under reduced pressure. The raw material was adsorbed on silica (dissolved in ethyl acetate), then purified by silica gel chromatography (cyclohexane: ethyl acetate gradient, the product was eluted at 80% of ethyl acetate) to afford additional title compound. ¹H NMR (400 MHz, DMSO-d₆) δ 11.85 (br. s., 1H), 7.32-7.44 (m, 3H), 7.09 (dd, J=3.8, 1.3 Hz, 1H), 6.66-6.77 (m, 3H), 5.67 (s, 2H). ¹³C NMR (400 MHz, DMSO-d₆) δ 154.15, 150.86, 137.98, 129.55, 123.98, 118.70, 116.65, 113.95, 113.32, 110.58.

Example 399E [4-(1-Oxo-1,2-dihydro-pyrrolo[1,2-d][1,2,4]triazin-4-yl)-phenyl]-carbamic acid phenyl ester

To a suspension of 50 mg 4-(4-aminophenyl)pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one (0.22 mmol) in 1 ml tetrahydrofuran at room temperature a solution of 0.03 ml pyridine (0.3 mmol) in 0.5 ml of tetrahydrofuran was added over 5 minutes. Subsequently, 0.03 ml phenylchlorformate (0.23 mmol) dissolved in 3 ml of tetrahydrofuran was added over 30 minutes and the reaction was stirred at room temperature overnight. The solvent was evaporated on vacuo and the mixture was directly incorporated on silica by dichloromethane. The mixture was purified by silica gel chromatography (4 g, cyclohexane:ethylacetate gradient) to afford crude material which was purified by column chromatography (cyclohexane:ethylacetate gradient) to afford the title compound.

Example 399F N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

40 mg [4-(1-Oxo-1,2-dihydro-pyrrolo[1,2-d][1,2,4]triazin-4-yl)-phenyl]-carbamic acid phenyl ester (0.115 mmol) were dissolved in 0.3 ml DMSO. A mixture of 15 mg isoindoline (0.121 mmol) in 0.2 ml DMSO was added at room temperature and the reaction was stirred at room temperature over night. The reaction mixture was diluted in ethyl acetate and washed with water, aqueous HCl, water, aqueous NaOH, and water. The solvent was evaporated under reduced pressure to afford the title compound.

Example 400 N-[4-(1-oxo-1,2-dihydropyrrolo[1,2-d][1,2,4]triazin-4-yl)phenyl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 400A 5-pyrrolidin-1-ylmethyl-1,3-dihydro-isoindole-2-carboxylic acid tert-butyl ester

To a solution of 1.25 g 5-hydroxymethyl-1,3-dihydro-isoindole-2-carboxylic acid tert-butyl ester (5.01 mmol) in 14 ml dichloromethane was slowly added 0.781 ml methanesulfonyl chloride (10.03 mmol) at room temperature. Subsequently the mixture was heated for 4 hours at reflux. LCMS control indicted a near complete formation of the corresponding mesylate, which was not isolated. After cooling to room temperature, 1.244 ml pyrrolidine (15.04 mmol) were added and the mixture was stirred at room temperature overnight. The reaction was complete according to LCMS. Water was added to the reaction mixture, the acidic aqueous phase was extracted two times with dichloromethane, and the water phase was basified and extracted three times with ethyl acetate. The combined ethyl acetate solutions were extracted with brine, dried over Na₂SO₄, filtered, and the organic solvent was removed under reduced pressure to provide the title compound. The dichloromethane phase was extracted two times with diluted NaOH, once with brine and then dried over Na₂SO₄. Filtration and removal of the organic solvent under reduced pressure provided additional title compound. Both fractions were combined and used in the next step without further purification. LCMS: m/z 303.2 (M+H).

Example 400B 5-pyrrolidin-1-ylmethyl-2,3-dihydro-1H-isoindole

To a solution of 1.90 g 5-pyrrolidin-1-ylmethyl-1,3-dihydro-isoindole-2-carboxylic acid tert-butyl ester (raw material; 4.96 mmol) in 5 ml dichloromethane was added 3.82 ml trifluoroacetic acid (49.6 mmol) and the reaction mixture was stirred at room temperature overnight. The trifluoroacetic acid and dichloromethane were evaporated under reduced pressure, water was added to the residue, the acidic aqueous phase extracted two times with ethyl acetate, the aqueous phase was basified with diluted NaOH and then subsequently extracted three times with dichloromethane. The dichloromethane phase was washed once with brine, dried over Na₂SO₄, filtered, and the solvent was removed under vacuum. The title compound was used without further purification in the next step. LCMS: m/z 203.2 (M+H).

Example 400C 5-pyrrolidin-1-ylmethyl-1,3-dihydro-isoindole-2-carboxylic acid [4-(1-oxo-1,2-dihydro-pyrrolo[1,2-d][1,2,4]triazin-4-yl)-phenyl]-amide

The title compound was prepared as described in Example 399E and Example 399F, substituting isoindoline with 5-pyrrolidin-1-ylmethyl-2,3-dihydro-1H-isoindole. LCMS: m/z 455.2 (M+H).

Example 401 tert-butyl 4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperidine-1-carboxylate

The title compound was prepared as described in Example 272A, substituting tert-butyl 4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}-3,6-dihydropyridine-1(2H)-carboxylate for 4-nitro-N-propylbenzamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), 7.46-7.48 (m, 2H), 7.34-7.39 (m, 2H), 7.28-7.33 (m, 2H), 7.10-7.13 (m, 2H), 4.75 (s, 4H), 4.02-4.08 (m, 2H), 2.71-2.90 (m, 2H), 2.57-2.68 (m, 1H), 1.71-1.76 (m, 2H), 1.40-1.51 (m, 2H), 1.42 (s, 9H); MS (ESI(−)) m/e 420 (M−H)⁻.

Example 402 N-[4-(5-propyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 402A N-(4-cyanophenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 4-isocyanatobenzonitrile for methyl 4-isocyanatobenzoate.

Example 402B (Z)—N-(4-(N′-hydroxycarbamimidoyl)phenyl)isoindoline-2-carboxamide

In a 25 mL pressure tube were mixed N-(4-cyanophenyl)isoindoline-2-carboxamide (500 mg, 1.899 mmol), hydroxylamine hydrochloride (264 mg, 3.80 mmol), and triethylamine (1.323 ml, 9.50 mmol) in ethanol (6 ml)/water (0.5 ml). The reaction vessel was sealed and heated at 80° C. for four hours. The reaction mixture was diluted with water and the solid was filtered off with water washes. HPLC purification provided the title compound.

Example 402C N-[4-(5-propyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

In a 4 mL vial was mixed (Z)—N-(4-(N′-hydroxycarbamimidoyl)phenyl)isoindoline-2-carboxamide (50 mg, 0.169 mmol), butyric acid (0.017 ml, 0.186 mmol), 1-hydroxybenzotriazole hydrate (12.92 mg, 0.084 mmol), and N-methylmorpholine (0.056 ml, 0.506 mmol) in anhydrous dimethylformamide (2 ml). To this solution was added N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (48.5 mg, 0.253 mmol) and the mixture was stirred overnight at ambient temperature. The solution was diluted with ethyl acetate and washed with water, saturated aqueous sodium bicarbonate, and brine. The organic layer was dried with sodium sulfate, decanted, and concentrated. The residue was taken up in anhydrous toluene (1 ml), and the mixture was heated at 110° C. for 2 days. The reaction was diluted with water; and the solids that formed were filtered and washed with water and ether to provide the title compound. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.68 (s, 1H), 7.89-7.91 (m, 2H), 7.78-7.80 (m, 2H), 7.36-7.40 (m, 2H), 7.30-7.34 (m, 2H), 4.76-4.85 (m, 4H), 2.96 (t, J=7.4 Hz, 2H), 1.81 (hex, J=7.4 Hz, 2H), 0.99 (t, J=7.4 Hz, 3H); MS (ESI(−)) m/e347 (M−H)⁻.

Example 403 N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}piperidine-1-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.28 (s, 1H), 7.46-7.48 (m, 2H), 7.34-7.37 (m, 2H), 7.30-7.33 (m, 2H), 7.09-7.12 (m, 2H), 4.75-4.76 (bs, 4H), 3.09-3.17 (m, 2H), 2.68 (td, J=12.3, 2.6 Hz, 2H), 2.57 (tt, J=12.0, 3.4 Hz, 1H), 1.71-1.75 (m, 2H), 1.56 (qd, J=12.5, 3.9 Hz, 2H); MS (ESI(+)) m/e 322 (M+H)⁺.

Example 404 N-{5-[((3R)-tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide and N-{5-[((3S)-tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (tetrahydrofuran-3-yl)methanamine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)nicotinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.26 (s, 1H), 8.74 (d, J=2.4 Hz, 1H), 8.56-8.60 (m, 1H), 8.14 (dd, J=8.8, 2.5 Hz, 1H), 8.00 (d, J=8.8 Hz, 1H), 7.26-7.40 (m, 4H), 4.59-5.02 (m, 4H), 3.75 (td, J=8.0, 5.7 Hz, 1H), 3.69 (dd, J=8.5, 6.9 Hz, 1H), 3.59-3.66 (m, 1H), 3.48 (dd, J=8.5, 5.2 Hz, 1H), 3.18-3.31 (m, 2H), 2.43-2.51 (m, 1H), 1.90-1.99 (m, 1H), 1.56-1.65 (m, 1H); MS (ESI(−)) m/e 365 (M−H)⁻.

Example 405 N-[4-(1-butyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting butyryl chloride for acetyl chloride and N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.27 (s, 1H), 7.46-7.49 (m, 2H), 7.34-7.39 (m, 2H), 7.28-7.33 (m, 2H), 7.11-7.14 (m, 2H), 4.75-4.76 (bs, 4H), 4.52-4.57 (m, 1H), 3.94-4.00 (m, 1H), 3.03-3.11 (m, 1H), 2.64-2.75 (m, 1H), 2.51-2.63 (m, 1H), 2.31 (t, J=7.4 Hz, 2H), 1.73-1.81 (m, 2H), 1.47-1.59 (m, 3H), 1.32-1.47 (m, 1H), 0.85-0.95 (m, 3H); MS (ESI(+)) m/e 392 (M+H)⁺.

Example 406 N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting isobutyryl chloride for acetyl chloride and N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.28 (s, 1H), 7.46-7.48 (m, 2H), 7.34-7.39 (m, 2H), 7.29-7.33 (m, 2H), 7.12-7.14 (m, 2H), 4.75-4.76 (bs, 4H), 4.53-4.58 (m, 1H), 4.03-4.07 (m, 1H), 3.06-3.14 (m, 1H), 2.86-2.93 (m, 1H), 2.67-2.74 (m, 1H), 2.53-2.61 (m, 1H), 1.75-1.84 (m, 2H), 1.45-1.56 (m, 1H), 1.33-1.45 (m, 1H), 1.03 (d, J=6.7 Hz, 3H), 1.00 (d, J=6.6 Hz, 3H); MS (ESI(−)) m/e 390 (M−H)⁻.

Example 407 N-[4-(1-benzoylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-[4-(piperidin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.29 (s, 1H), 7.47-7.50 (m, 2H), 7.41-7.47 (m, 5H), 7.34-7.38 (m, 2H), 7.29-7.33 (m, 2H), 7.16-7.18 (m, 2H), 4.75-4.76 (bs, 4H), 4.54-4.64 (m, 1H), 3.57-3.74 (m, 1H), 3.02-3.21 (m, 1H), 2.79-2.93 (m, 1H), 2.75 (tt, J=11.9, 3.4 Hz, 1H), 1.68-1.88 (m, 2H), 1.54-1.63 (m, 2H); MS (ESI(−)) m/e 424 (M−H)⁻.

Example 408 N-{4-[5-(3-methylbutyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 402C, substituting 4-methylpentanoic acid for butyric acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.69 (s, 1H), 7.89-7.91 (m, 2H), 7.77-7.79 (m, 2H), 7.36-7.39 (m, 2H), 7.31-7.34 (m, 2H), 4.80-4.81 (bs, 4H), 2.96-3.00 (m, 2H), 1.66-1.72 (m, 2H), 1.59-1.67 (m, 1H), 0.93 (d, J=6.4 Hz, 6H); MS (ESI(−)) m/e 375 (M−H)⁻.

Example 409 N-[4-(5-benzyl-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 402C, substituting phenylacetic acid for butyric acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.69 (s, 1H), 7.87-7.90 (m, 2H), 7.77-7.79 (m, 2H), 7.35-7.42 (m, 6H), 7.29-7.34 (m, 3H), 4.75-4.84 (m, 4H), 4.42 (s, 2H); MS (ESI(+)) m/e 397 (M+H)⁺.

Example 410 N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

A racemic mixture of N-(4-{[tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide (250 mg) was dissolved in methanol and separated using SCF-LC with a ChiralPak AD-H 21×250 mm column to provide N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.58 (s, 1H), 8.38 (t, J=5.7 Hz, 1H), 7.75-7.79 (m, 2H), 7.64-7.69 (m, 2H), 7.30-7.41 (m, 4H), 4.78-4.79 (bs, 4H), 3.57-3.78 (m, 3H), 3.48 (dd, J=8.5, 5.2 Hz, 1H), 3.17-3.28 (m, 2H), 2.41-2.50 (m, 1H), 1.87-2.04 (m, 1H), 1.54-1.66 (m, 1H); MS (ESI(+)) m/e 366 (M+H)⁺.

Example 411 N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

A racemic mixture of N-(4-{[tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide (250 mg) was dissolved in methanol and separated using SCF-LC with a ChiralPak AD-H 21×250 mm column to provide N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (s, 1H), 8.38 (t, J=5.7 Hz, 1H), 7.75-7.79 (m, 2H), 7.64-7.69 (m, 2H), 7.30-7.39 (m, 4H), 4.78-4.79 (bs, 4H), 3.57-3.78 (m, 3H), 3.48 (dd, J=8.5, 5.3 Hz, 1H), 3.13-3.29 (m, 2H), 2.40-2.50 (m, 1H), 1.87-2.07 (m, 1H), 1.54-1.66 (m, 1H); MS (ESI(+)) m/e 366 (M+H)⁺.

Example 422 tert-butyl 4-{6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]-1H-benzimidazol-2-yl}piperazine-1-carboxylate Example 422A tert-butyl 4-(5-nitro-1H-benzo[d]imidazol-2-yl)piperazine-1-carboxylate

In a 20 mL sealed tube under nitrogen, a mixture of tert-butyl piperazine-1-carboxylate (0.943 g, 5.06 mmol), 2-chloro-5-nitro-1H-benzo[d]imidazole (0.5 g, 2.53 mmol) and ethanol (9.5 mL) was heated at 135° C. for 2 hours. The reaction was concentrated and the residue was purified by reverse-phase chromatography to provide the title compound.

Example 422B tert-butyl 4-(5-amino-1H-benzo[d]imidazol-2-yl)piperazine-1-carboxylate

The title compound was prepared as described in Example 274, substituting tert-butyl 4-(5-nitro-1H-benzo[d]imidazol-2-yl)piperazine-1-carboxylate for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 422C tert-butyl 4-{6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]-1H-benzimidazol-2-yl}piperazine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(5-amino-1H-benzo[d]imidazol-2-yl)piperazine-1-carboxylate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 10.90-11.08 (bs, 1H), 7.84-7.85 (m, 1H), 7.46-7.48 (m, 1H), 7.27-7.35 (m, 4H), 7.04-7.06 (m, 2H), 4.76 (s, 4H), 3.46 (s, 8H), 1.44 (s, 9H); MS (ESI(+)) m/e 463 (M+H)⁺.

Example 423 N-[2-(piperazin-1-yl)-1H-benzimidazol-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-{6-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]-1H-benzimidazol-2-yl}piperazine-1-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 11.04-11.29 (m, 1H), 8.08-8.12 (bs, 1H), 7.41-7.58 (m, 1H), 7.24-7.39 (m, 4H), 7.04-7.06 (m, 2H), 4.76 (s, 4H), 3.37-3.44 (m, 4H), 2.85-2.89 (m, 4H); MS (ESI(+)) m/e 363 (M+H)⁺.

Example 424 N-[4-(propylcarbamoyl)phenyl]-5-vinyl-1,3-dihydro-2H-isoindole-2-carboxamide

In a sealed vial under nitrogen, a mixture of potassium vinyltrifluoroborate (100 mg, 0.75 mmol), 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide (150 mg, 0.37 mmol), bis(triphenylphosphine)palladium(II) chloride and saturated aqueous sodium bicarbonate (0.62 ml) in dimethylformamide was heated at 85° C. for 5 hours. The reaction was poured into water, filtered, dried and purified by reverse-phase chromatography to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (s, 1H), 8.25 (t, J=5.7 Hz, 1H), 7.75-7.78 (m, 2H), 7.63-7.67 (m, 2H), 7.47 (s, 1H), 7.42 (dd, J=7.9, 1.5 Hz, 1H), 7.34 (d, J=7.8 Hz, 1H), 6.77 (dd, J=17.6, 10.9 Hz, 1H), 5.85 (dd, J=17.6, 1.0 Hz, 1H), 5.27 (d, J=11.0 Hz, 1H), 4.77-4.78 (bs, 4H), 3.16-3.22 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 350 (M+H)⁺.

Example 428 N-{4-[5-(tetrahydrofuran-3-yl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 402C, substituting tetrahydrofuran-3-carboxylic acid for butyric acid. ¹H NMR (500 MHz, DMSO-d₆)₆ ppm 8.69 (s, 1H), 7.89-7.92 (m, 2H), 7.78-7.81 (m, 2H), 7.36-7.40 (m, 2H), 7.30-7.34 (m, 2H), 4.80-4.81 (bs, 4H), 4.08 (dd, J=8.6, 7.6 Hz, 1H), 3.97 (dd, J=8.6, 5.4 Hz, 1H), 3.86-3.95 (m, 2H), 3.79-3.85 (m, 1H), 2.40 (dddd, J=12.5, 9.0, 7.6, 5.9 Hz, 1H), 2.26 (ddt, J=7.7, 12.4, 6.2 Hz, 1H); MS (ESI(−)) m/e 375 (M−H)⁻.

Example 429 N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

In a 4 mL were mixed N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide (50 mg, 0.157 mmol) and isobutyraldehyde (0.014 ml, 0.157 mmol) in anhydrous dichloroethane (2 ml) at room temperature. Sodium triacetoxyborohydride (46.4 mg, 0.219 mmol) was added, and reaction was stirred overnight. The reaction mixture was diluted with water, ethyl acetate and saturated aqueous sodium bicarbonate. The layers were separated and the organic layer was washed with brine. The organic layer was diluted with methanol, dried with sodium sulfate, filtered and concentrated. The residue was purified by flash chromatography to provide the title compound. ¹H NMR (400 MHz, DMSO-d₆) 0.5 ppm 8.35 (s, 1H), 7.53-7.55 (m, 2H), 7.30-7.38 (m, 6H), 6.06-6.08 (m, 1H), 4.77 (s, 4H), 3.01-3.03 (m, 2H), 2.57 (t, J=5.6 Hz, 2H), 2.41-2.47 (m, 2H), 2.14 (d, J=7.3 Hz, 2H), 1.77-1.88 (m, 1H), 0.88 (d, J=6.5 Hz, 6H); MS (ESI(−)) m/e 374 (M−H)⁻.

Example 432 N-{4-[1-(4-methylbenzoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting 4-methylbenzoyl chloride for acetyl chloride and N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) 0.5 ppm 8.38 (s, 1H), 7.55-7.58 (m, 2H), 7.20-7.39 (m, 10H), 6.01-6.21 (m, 1H), 4.77 (s, 4H), 3.93-4.36 (m, 2H), 3.43-3.90 (m, 2H), 2.48-2.57 (m, 2H), 2.36 (s, 3H); MS (ESI(+)) m/e 438 (M+H)⁺.

Example 433 N-[4-(1-benzyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 429, substituting benzaldehyde for isobutyraldehyde. ¹H NMR (400 MHz, DMSO-d₆) 0.5 ppm 8.36 (s, 1H), 7.52-7.55 (m, 2H), 7.20-7.42 (m, 11H), 6.06-6.08 (m, 1H), 4.76-4.77 (bs, 4H), 3.58 (s, 2H), 3.04-3.06 (m, 2H), 2.63 (t, J=5.6 Hz, 2H), 2.42-2.49 (m, 2H); MS (ESI(+)) m/e 410 (M+H)⁺.

Example 440 N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting pyridin-3-ylboronic acid for 1H-pyrazol-3-ylboronic acid and 5-bromo-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.91 (dd, J=2.4, 0.9 Hz, 1H), 8.63 (s, 1H), 8.58 (dd, J=4.7, 1.6 Hz, 1H), 8.27 (t, J=5.6 Hz, 1H), 8.10 (ddd, J=7.9, 2.4, 1.6 Hz, 1H), 7.73-7.79 (m, 3H), 7.65-7.70 (m, 3H), 7.48-7.53 (m, 2H), 4.79-4.91 (m, 4H), 3.15-3.23 (m, 2H), 1.54 (s, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 401 (M+H)⁺.

Example 441 N-{4-[(propylamino)carbonyl]phenyl}-5-pyridin-4-yl-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting pyridin-4-ylboronic acid for 1H-pyrazol-3-ylboronic acid and 5-bromo-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.62-8.66 (m, 3H), 8.25 (t, J=5.6 Hz, 1H), 7.70-7.81 (m, 6H), 7.64-7.69 (m, 2H), 7.52 (d, J=8.0 Hz, 1H), 4.85-4.92 (m, 4H), 3.16-3.22 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H). MS (ESI(+)) m/e 401 (M+H)⁺.

Example 442 N⁵-(2-methoxyethyl)-N²-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide

The title compound was prepared as described in Example 1C, substituting 2-methoxyethanamine for 3-phenylpropan-1-amine and 2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), 8.54 (d, J=5.3 Hz, 1H), 8.26 (t, J=5.7 Hz, 1H), 7.79-7.85 (m, 2H), 7.73-7.80 (m, 2H), 7.63-7.67 (m, 2H), 7.45 (d, J=7.8 Hz, 1H), 4.81-4.83 (bs, 4H), 3.39-3.51 (m, 4H), 3.27 (s, 3H), 3.03-3.22 (m, 2H), 1.46-1.59 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 425 (M+H)⁺.

Example 443 N-(4-cyanophenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 4-isocyanatobenzonitrile for methyl 4-isocyanatobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.83 (s, 1H), 7.78-7.82 (m, 2H), 7.69-7.73 (m, 2H), 7.31-7.39 (m, 4H), 4.79-4.81 (bs, 4H); MS (ESI(+)) m/e 264 (M+H)⁺.

Example 444 N-[4-(trifluoromethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 1-isocyanato-4-(trifluoromethyl)benzene for methyl 4-isocyanatobenzoate. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.74 (s, 1H), 7.80-7.83 (m, 2H), 7.60-7.63 (m, 2H), 7.30-7.39 (m, 4H), 4.79-4.80 (bs, 4H); MS (ESI(+)) m/e 307 (M+H)⁺.

Example 450 5-(1,2-dihydroxyethyl)-N-{4-[(propylamino)carbonyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

A suspension of N-[4-(propylcarbamoyl)phenyl]-5-vinyl-1,3-dihydro-2H-isoindole-2-carboxamid (0.03 g, 0.086 mmol) in tetrahydrofuran (1 ml) and 2-propanol (0.3 ml) was treated with osmium tetroxide (2.5% wt. % solution in 2-methyl-2-propanol) (0.108 ml, 8.59 μmol). The reaction mixture was treated with N-methylmorpholine-N-oxide (0.030 g, 0.258 mmol). The reaction mixture was allowed to stir at room temperature overnight, quenched with aqueous sodium sulfite solution and extracted with ethyl acetate. The combined organic layers were washed with brine, dried over anhydrous sodium sulfate, and concentrated under vacuum. Flash chromatography provided the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (s, 1H), 8.25 (t, J=5.7 Hz, 1H), 7.74-7.78 (m, 2H), 7.63-7.68 (m, 2H), 7.27-7.33 (m, 3H), 5.24 (d, J=4.2 Hz, 1H), 4.75-4.77 (bs, 4H), 4.70 (t, J=5.8 Hz, 1H), 4.53-4.59 (m, 1H), 3.43 (t, J=5.8 Hz, 2H), 3.16-3.23 (m, 2H), 1.42-1.63 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 384 (M+H)⁺.

Example 451 N-[4-(1-benzoylpiperidin-4-yl)butyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide Example 451A tert-butyl 4-(4-(5-cyanoisoindoline-2-carboxamido)butyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(4-aminobutyl)piperidine-1-carboxylate for 4-amino-N-propylbenzamide and isoindoline-5-carbonitrile for methyl isoindoline-5-carboxylate hydrochloride.

Example 451B 5-cyano-N-(4-(piperidin-4-yl)butyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(5-cyanoisoindoline-2-carboxamido)butyl)piperidine-1-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 451C N-[4-(1-benzoylpiperidin-4-yl)butyl]-5-cyano-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and 5-cyano-N-(4-(piperidin-4-yl)butyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.83 (s, 1H), 7.75 (dd, J=7.9, 1.5 Hz, 1H), 7.53 (d, J=7.9 Hz, 1H), 7.41-7.44 (m, 3H), 7.31-7.38 (m, 2H), 6.36 (t, J=5.5 Hz, 1H), 4.60-4.64 (m, 4H), 4.30-4.53 (m, 1H), 3.42-3.71 (m, 1H), 3.02-3.10 (m, 2H), 2.64-3.00 (m, 2H), 1.56-1.84 (m, 2H), 1.37-1.54 (m, 3H), 1.24-1.31 (m, 4H), 0.93-1.16 (m, 2H); MS (ESI(+)) m/e 431 (M+H)⁺.

Example 452 N-(1′-butyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 452A N-(5-bromopyridin-2-yl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 344A, substituting 5-bromopyridin-2-amine for tert-butyl 5-aminoisoindoline-2-carboxylate.

Example 452B tert-butyl 4-(6-(isoindoline-2-carboxamido)pyridin-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 280, substituting tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for 1H-pyrazol-3-ylboronic acid and N-(5-bromopyridin-2-yl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide.

Example 452C N-(5-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-2-yl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(6-(isoindoline-2-carboxamido)pyridin-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 452D N-(1′-butyryl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting butyryl chloride for acetyl chloride and N-(5-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-2-yl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.92-8.95 (bs, 1H), 8.32-8.35 (m, 1H), 7.64-7.97 (m, 2H), 6.94-7.38 (m, 4H), 6.16-6.22 (bs, 1H), 4.45-5.02 (m, 4H), 4.08-4.15 (m, 2H), 3.62-3.68 (m, 2H), 2.23-2.65 (m, 4H), 1.46-1.64 (m, 2H), 0.87-0.93 (m, 3H); MS (ESI(+)) m/e 391 (M+H)⁺.

TABLE 6 The title compound was prepared as described in Example 1C, substituting N-(5- (1,2,3,6-tetrahydropyridin-4-yl)pyridin-2-yl)isoindoline-2-carboxamide for 3-phenylpropanl- amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 453 N-(1′-isobutyryl- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.91-8.95 (bs, (ESI(+)) 1′,2′,3′,6′-tetrahydro- 1H), 8.33-8.38 (m, 1H), 7.79-7.92 (m, 2H), m/e 391 3,4′-bipyridin-6-yl)-1,3- 7.27-7.36 (m, 3H), 6.17-6.22 (bs, 1H), 4.76-4.83 (bs, 4H), (M + H)⁺ dihydro-2H-isoindole-2- 4.07-4.22 (m, 2H), 3.64-3.73 (m, 1H), 2.84-2.98 (m, 1H), carboxamide 2.37-2.63 (m, 3H), 0.77-1.20 (m, 6H) 454 N-[1′-((3R)- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.92-8.95 (bs, (ESI(+)) tetrahydrofuran-3- 1H), 8.32-8.36 (bs, 1H), 7.79-7.92 (m, 2H), m/e 419 ylcarbonyl)-1′,2′,3′,6′- 7.11-7.51 (m, 4H), 6.17-6.21 (bs, 1H), 4.59-5.04 (m, 4H), (M + H)⁺ tetrahydro-3,4′- 4.10-4.22 (m, 2H), 3.82-4.01 (m, 1H), 3.59-3.81 (m, 5H), bipyridin-6-yl]-1,3- 2.33-2.62 (m, 2H), 1.94-2.15 (m, 2H) dihydro-2H-isoindole-2- carboxamide 495 N-(1′-benzoyl-1′,2′,3′,6′- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) tetrahydro-3,4′- 8.51 (bs, 1H), 8.32 (d, J = 2.5 Hz, 1H), 7.90 (d, J = 8.7 Hz, m/e 425 bipyridin-6-yl)-1,3- 1H), 7.77 (dd, J = 8.7, 2.5 Hz, 1H), (M + H)⁺ dihydro-2H-isoindole-2- 7.48-7.39 (m, 5H), 7.36-7.25 (m, 4H), 6.16 (bs, 1H), carboxamide 4.81 (s, 4H), 4.18 (m, 2H), 3.68 (m, 2H), 2.55 (m, 2H) 764 N-[1′-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) 2-ylcarbonyl)-1′,2′,3′,6′- 8.52 (bs, 1H), 8.32 (d, J = 2.5 Hz, 1H), 7.91 (m, 1H), m/e 419 tetrahydro-3,4′- 7.76 (dd, J = 8.7, 2.5 Hz, 1H), 7.37-7.26 (m, 4H), (M + H)⁺ bipyridin-6-yl]-1,3- 6.16 (m, 1H), 4.82 (s, 4H), 4.68 (dd, J = 7.6, 5.6 Hz, dihydro-2H-isoindole-2- 1H), 4.17 (m, 2H), 3.86-3.70 (m, 4H), 2.52 (m, 2H), carboxamide 2.12 (m, 1H), 2.01 (m, 1H), 1.87 (m, 2H) 765 N-[1′-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) pyran-4-ylcarbonyl)- 8.52 (s, 1H), 8.32 (d, J = 2.5 Hz, 1H), 7.91 (d, J = 8.7 Hz, m/e 433 1′,2′,3′,6′-tetrahydro- 1H), 7.77 (dd, J = 8.7, 2.5 Hz, 1H), (M + H)⁺ 3,4′-bipyridin-6-yl]-1,3- 7.37-7.26 (m, 4H), 6.16 (m, 1H), 4.82 (s, 4H), 4.17 (m, 2H), dihydro-2H-isoindole-2- 3.87 (m, 2H), 3.72 (t, J = 5.7 Hz, 2H), 3.43 (td, J = 11.4, carboxamide 2.6 Hz, 2H), 2.92 (m 1H), 2.52 (m, 2H), 1.74-1.60 (m, 2H), 1.62-1.53 (m, 2H) 766 N-[1′-(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) ylcarbonyl)-1′,2′,3′,6′- 8.52 (s, 1H), 8.32 (d, J = 2.2 Hz, 1H), 7.91 (d, J = 8.8 Hz, m/e 435 tetrahydro-3,4′- 1H), 7.76 (dd, J = 8.8, 2.5 Hz, 1H), (M + H)⁺ bipyridin-6-yl]-1,3- 7.40-7.23 (m, 4H), 6.15 (m, 1H), 4.82 (s, 4H), 4.38 (dd, J = 9.2, dihydro-2H-isoindole-2- 2.9 Hz, 1H), 4.16 (m, 2H), 3.83-3.61 (m, 7H), carboxamide 3.53 (m, 1H), 2.53 (m, 2H) 767 N-{1′-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) methylpyrrolidin-3- 8.54 (m, 1H), 8.31 (dd, J = 2.5, 0.8 Hz, 1H), 7.90 (dd, m/e 432 yl)carbonyl]-1′,2′,3′,6′- J = 8.7, 0.8 Hz, 1H), 7.75 (dd, J = 8.7, 2.5 Hz, 1H), (M + H)⁺ tetrahydro-3,4′- 7.36-7.25 (m, 4H), 6.15 (m, 1H), 4.81 (s, 4H), bipyridin-6-yl}-1,3- 4.13 (m, 2H), 3.69 (t, J = 5.7 Hz, 2H), 3.26 (m, 1H), dihydro-2H-isoindole-2- 2.77 (t, J = 8.6 Hz, 1H), 2.68-2.53 (m, 4H), 2.38 (m, 1H), carboxamide 2.24 (s, 3H), 2.13-1.92 (m, 2H) 768 N-{1′-[(1,1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) dioxidotetrahydrothiophen- 8.53 (bs, 1H), 8.33 (d, J = 2.5 Hz, 1H), 7.91 (d, J = 8.7 Hz, m/e 467 3-yl)carbonyl]- 1H), 7.77 (dd, J = 8.7, 2.5 Hz, 1H), (M + H)⁺ 1′,2′,3′,6′-tetrahydro- 7.37-7.26 (m, 4H), 6.16 (m, 1H), 4.82 (s, 4H), 4.19 (m, 3,4′-bipyridin-6-yl}-1,3- 2H), 3.74 (m, 3H), 3.33-3.05 (m, 4H), 2.55 (m, 2H), dihydro-2H-isoindole-2- 2.37 (m, 1H), 2.15 (m, 1H) carboxamide 769 N-[1′-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) methylpropanoyl)- 8.51 (bs, 1H), 8.31 (d, J = 2.5 Hz, 1H), 7.90 (d, J = 8.7 Hz, m/e 407 1′,2′,3′,6′-tetrahydro- 1H), 7.76 (dd, J = 8.7, 2.5 Hz, 1H), (M + H)⁺ 3,4′-bipyridin-6-yl]-1,3- 7.36-7.25 (m, 4H), 6.17 (m, 1H), 5.11 (bs, 1H), 4.81 (s, dihydro-2H-isoindole-2- 4H), 4.30 (m, 2H), 3.94 (m, 2H), 2.51 (m, 2H), carboxamide 1.37 (s, 6H) 801 N-[1′-(morpholin-4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ ppm (ESI(+)) ylacetyl)-1′,2′,3′,6′- 8.51 (s, 1H), 8.32 (d, J = 2.5 Hz, 1H), 7.90 (d, J = 8.7 Hz, m/e 448 tetrahydro-3,4′- 1H), 7.76 (dd, J = 8.7, 2.5 Hz, 1H), (M + H)⁺ bipyridin-6-yl]-1,3- 7.36-7.26 (m, 4H), 6.15 (m, 1H), 4.81 (s, 4H), 4.13 (m, 2H), dihydro-2H-isoindole-2- 3.73 (m, 2H), 3.58 (m, 4H), 3.21 (s, 2H), 2.48 (m, carboxamide 2H), 2.45 (m, 4H)

Example 455 N-[2-(4-acetylpiperazin-1-yl)-1H-benzimidazol-5-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting N-[2-(piperazin-1-yl)-1H-benzimidazol-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (500 MHz, DMSO-d₆, Temp=90° C.) δ ppm 11.01-11.10 (bs, 1H), 7.89-7.91 (bs, 1H), 7.44-7.52 (m, 1H), 7.32-7.35 (m, 2H), 7.27-7.31 (m, 2H), 7.03-7.06 (m, 2H), 4.76 (s, 4H), 3.55-3.62 (m, 4H), 3.46-3.51 (m, 4H), 2.04 (s, 3H); MS (ESI(+)) m/e 405 (M+H)⁺.

TABLE 7 The following Examples were essentially prepared as described in Example 1C, substituting the appropriate tetrahdropyridine for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 456 N-{4-[1-(5-oxo-L- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(−)) m/e prolyl)-1,2,3,6- ppm 8.15-8.17 (bs, 1H), 7.85-7.88 (m, 3H), 429 (M − H)⁻ tetrahydropyridin-4- 7.36-7.38 (m, 2H), 7.16-7.25 (m, 4H), 5.97-5.99 (m, yl]phenyl}-1,3-dihydro- 1H), 4.85-4.88 (m, 4H), 4.60-4.64 (m, 1H), 2H-isoindole-2- 4.09-4.26 (m, 2H), 3.57-3.81 (m, 2H), 2.40-2.50 (m, carboxamide 3H), 2.25-2.38 (m, 2H), 2.08-2.15 (m, 1H) 457 N-{4-[1-(5-oxo-D- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(−)) m/e prolyl)-1,2,3,6- ppm 8.14-8.16 (bs, 1H), 7.85-7.88 (m, 2H), 429 (M − H)⁻ tetrahydropyridin-4- 7.75-7.82 (m, 1H), 7.36-7.38 (m, 2H), 7.20-7.24 (m, yl]phenyl}-1,3-dihydro- 2H), 7.16-7.20 (m, 2H), 5.97-5.99 (m, 1H), 2H-isoindole-2- 4.83-4.89 (m, 4H), 4.60-4.63 (m, 1H), 3.59-3.79 (m, carboxamide 2H), 2.40-2.51 (m, 3H), 2.24-2.38 (m, 2H), 2.08-2.15 (m, 1H) 458 N-[4-(1-propionyl- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) 1,2,3,6-tetrahydropyridin- ppm 8.08-8.15 (m, 1H), 7.84-7.87 (m, 2H), m/e 376 4-yl)phenyl]-1,3-dihydro- 7.37-7.39 (m, 2H), 7.20-7.24 (m, 2H), 7.16-7.19 (m, (M + H)⁺ 2H-isoindole-2- 2H), 5.99 (t, J = 3.2 Hz, 1H), 4.84-4.87 (m, 4H), carboxamide 4.08-4.22 (m, 2H), 3.55-3.75 (m, 2H), 2.42-2.49 (m, 2H), 2.31 (q, J = 7.4 Hz, 2H), 1.17 (t, J = 7.5 Hz, 3H) 459 N-{4-[1-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methylbutanoyl)-1,2,3,6- ppm 8.11-8.12 (bs, 1H), 7.84-7.86 (m, 2H), m/e 404 tetrahydropyridin-4- 7.38-7.40 (m, 2H), 7.20-7.24 (m, 2H), 7.18 (d, J = 4.1 Hz, (M + H)⁺ yl]phenyl}-1,3-dihydro- 1H), 7.15-7.18 (m, 1H), 6.00-6.03 (m, 1H), 2H-isoindole-2- 4.83-4.89 (m, 4H), 4.18-4.27 (m, 2H), carboxamide 3.67-3.79 (m, 2H), 2.69 (h, J = 6.7 Hz, 1H), 2.48-2.51 (m, 2H), 1.75-1.89 (m, 1H), 1.40-1.53 (m, 1H), 1.15 (d, J = 6.9 Hz, 3H), 0.90 (t, J = 7.4 Hz, 3H) 460 N-{4-[1-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ethylbutanoyl)-1,2,3,6- ppm 8.12 (d, J = −1.9 Hz, 1H), 7.84-7.87 (m, 2H), m/e 418 tetrahydropyridin-4- 7.38-7.41 (m, 2H), 7.21-7.24 (m, 2H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.15-7.20 (m, 2H), 6.01-6.04 (m, 1H), 4.86 (s, 4H), 2H-isoindole-2- 4.21-4.32 (m, 2H), 3.73-3.84 (m, 2H), 2.57-2.67 (m, 1H), carboxamide 2.48-2.55 (m, 2H), 1.74-1.88 (m, 2H), 1.45-1.57 (m, 2H), 0.90 (t, J = 7.4 Hz, 6H) 461 N-{4-[1-(methoxyacetyl)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 1,2,3,6-tetrahydropyridin- ppm 2.48-2.54 (m, 2H), 3.32 (s, 3H), 3.64 (t, m/e 392 4-yl]phenyl}-1,3- J = 5.80 Hz, 2H), 4.06-4.13 (m, 4H), 4.77 (s, 4H), (M + H)⁺ dihydro-2H-isoindole-2- 6.02-6.09 (m, 1H), 7.27-7.37 (m, 6H), carboxamide 7.51-7.56 (m, 2H), 8.12 (s, 1H) 462 N-{4-[1-(ethoxyacetyl)- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) 1,2,3,6-tetrahydropyridin- ppm 8.11-8.12 (bs, 1H), 7.84-7.86 (m, 2H), m/e 406 4-yl]phenyl}-1,3- 7.36-7.39 (m, 2H), 7.20-7.25 (m, 2H), 7.13-7.20 (m, (M + H)⁺ dihydro-2H-isoindole-2- 2H), 5.97-6.00 (m, 1H), 4.84-4.88 (m, 4H), 4.24 (s, carboxamide 2H), 4.18-4.23 (m, 2H), 3.69-3.74 (m, 2H), 3.57 (q, J = 6.9 Hz, 2H), 2.46-2.53 (m, 2H), 1.17 (t, J = 6.9 Hz, 3H) 463 N-(4-{1-[(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methoxyethoxy)acetyl]- ppm 8.10-8.13 (bs, 1H), 7.82-7.87 (m, 2H), m/e 436 1,2,3,6-tetrahydropyridin- 7.35-7.40 (m, 2H), 7.19-7.25 (m, 2H), 7.15-7.20 (m, (M + H)⁺ 4-yl}phenyl)-1,3- 2H), 5.96-6.00 (m, 1H), 4.84-4.88 (m, 4H), dihydro-2H-isoindole-2- 4.30-4.34 (m, 2H), 4.17-4.25 (m, 2H), 3.73-3.77 (m, carboxamide 2H), 3.67-3.76 (m, 2H), 3.54-3.58 (m, 2H), 3.28 (s, 3H), 2.46-2.53 (m, 2H) 464 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) 2-ylcarbonyl)-1,2,3,6- ppm 8.08-8.14 (bs, 1H), 7.82-7.87 (m, 2H), m/e 418 tetrahydropyridin-4- 7.34-7.40 (m, 2H), 7.20-7.25 (m, 2H), 7.15-7.20 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 5.97-6.01 (m, 1H), 4.83-4.89 (m, 4H), 2H-isoindole-2- 4.69 (dd, J = 7.2, 5.3 Hz, 1H), 4.24-4.31 (m, 2H), carboxamide 3.87-3.96 (m, 1H), 3.69-3.88 (m, 3H), 2.39-2.60 (m, 3H), 1.84-2.01 (m, 2H), 1.69-1.83 (m, 1H) 465 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(−)) m/e 3-ylcarbonyl)-1,2,3,6- ppm 8.12-8.14 (bs, 1H), 7.83-7.89 (m, 2H), 416 (M − H)⁻ tetrahydropyridin-4- 7.38-7.40 (m, 2H), 7.20-7.24 (m, 2H), 7.15-7.20 (m, yl]phenyl}-1,3-dihydro- 2H), 5.99-6.02 (m, 1H), 4.83-4.89 (m, 4H), 2H-isoindole-2- 4.16-4.24 (m, 2H), 4.04-4.13 (m, 2H), 3.91 (td, J = 7.9, carboxamide 5.9 Hz, 1H), 3.77-3.83 (m, 1H), 3.60-3.79 (m, 2H), 3.23-3.35 (m, 1H), 2.42-2.49 (m, 2H), 2.29 (ddd, J = 7.6, 12.1, 6.1 Hz, 1H), 1.97-2.06 (m, 1H) 466 N-{4-[1- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) (cyclopropylacetyl)- ppm 8.11-8.12 (bs, 1H), 7.84-7.87 (m, 2H), m/e 402 1,2,3,6-tetrahydropyridin- 7.37-7.40 (m, 2H), 7.20-7.23 (m, 2H), 7.15-7.20 (m, (M + H)⁺ 4-yl]phenyl}-1,3- 2H), 5.99-6.01 (m, 1H), 4.86 (s, 4H), 4.10-4.28 (m, dihydro-2H-isoindole-2- 2H), 3.55-3.77 (m, 2H), 2.43-2.52 (m, 2H), 2.36 (d, carboxamide J = 6.5 Hz, 2H), 1.13-1.24 (m, 1H), 0.48-0.54 (m, 2H), 0.19-0.27 (m, 2H) 467 N-{4-[1- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) (cyclopentylcarbonyl)- ppm 8.10-8.13 (bs, 1H), 7.83-7.88 (m, 2H), m/e 416 1,2,3,6-tetrahydropyridin- 7.38-7.41 (m, 2H), 7.21-7.24 (m, 2H), 7.15-7.20 (m, (M + H)⁺ 4-yl]phenyl}-1,3- 2H), 6.00-6.03 (m, 1H), 4.83-4.87 (m, 4H), dihydro-2H-isoindole-2- 4.16-4.26 (m, 2H), 3.63-3.83 (m, 2H), 2.96 (s, 1H), carboxamide 2.44-2.52 (m, 2H), 1.92-2.04 (m, 2H), 1.75-1.87 (m, 2H), 1.65-1.75 (m, 2H), 1.46-1.60 (m, 2H) 468 N-{4-[1-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methylbenzoyl)-1,2,3,6- ppm 8.12-8.13 (bs, 1H), 7.84-7.87 (m, 3H), m/e 438 tetrahydropyridin-4- 7.37-7.40 (m, 3H), 7.21-7.30 (m, 5H), 5.94-6.05 (bs, (M + H)⁺ yl]phenyl}-1,3-dihydro- 1H), 4.86 (s, 4H), 4.86 (s, 1H), 4.19-4.48 (m, 2H), 2H-isoindole-2- 3.35-3.61 (m, 2H), 2.39-2.59 (m, 2H), 2.32 (s, 3H) carboxamide 469 N-{4-[1-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methylbenzoyl)-1,2,3,6- ppm 8.11-8.13 (bs, 1H), 7.84-7.87 (m, 2H), m/e 438 tetrahydropyridin-4- 7.34-7.41 (m, 4H), 7.28 (t, J = 7.5 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.20-7.24 (m, 2H), 7.17-7.19 (m, 3H), 5.98-6.01 (bs, 1H), 2H-isoindole-2- 4.83-4.90 (m, 4H), 4.26-4.29 (m, 2H), carboxamide 3.70-3.79 (m, 2H), 2.50-2.54 (m, 2H), 2.26 (s, 3H) 470 N-{4-[1-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methoxybenzoyl)-1,2,3,6- ppm 8.11-8.12 (bs, 1H), 7.83-7.86 (m, 2H), m/e 454 tetrahydropyridin-4- 7.37-7.45 (m, 3H), 7.30-7.35 (m, 1H), 7.20-7.23 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.15-7.19 (m, 2H), 7.00 (t, J = 7.4 Hz, 1H), 2H-isoindole-2- 6.96 (d, J = 8.3 Hz, 1H), 5.89-6.08 (m, 1H), 4.85 (s, carboxamide 4H), 4.31-4.68 (m, 2H), 3.69 (s, 3H), 3.28-3.62 (m, 2H), 2.34-2.68 (m, 2H) 471 N-{4-[1-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methoxybenzoyl)-1,2,3,6- ppm 8.11-8.13 (bs, 1H), 7.84-7.87 (m, 2H), m/e 454 tetrahydropyridin-4- 7.37-7.40 (m, 2H), 7.30-7.34 (m, 1H), 7.20-7.24 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 3H), 7.16-7.19 (m, 2H), 7.12-7.15 (m, 1H), 2H-isoindole-2- 7.01 (ddd, J = 8.2, 2.6, 1.0 Hz, 1H), 5.98-6.00 (bs, 1H), carboxamide 4.84-4.89 (m, 4H), 4.26-4.29 (m, 2H), 3.71-3.78 (m, 2H), 3.69 (s, 3H), 2.49-2.54 (m, 2H) 472 N-{4-[1-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methoxybenzoyl)-1,2,3,6- ppm 8.11-8.12 (bs, 1H), 7.84-7.87 (m, 2H), m/e 454 tetrahydropyridin-4- 7.55-7.58 (m, 2H), 7.38-7.41 (m, 2H), 7.20-7.24 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.16-7.19 (m, 2H), 6.97-6.99 (m, 2H), 2H-isoindole-2- 5.99-6.02 (m, 1H), 4.86 (s, 4H), 4.29 (q, J = 2.9 Hz, 2H), carboxamide 3.77 (t, J = 5.7 Hz, 2H), 3.71 (s, 3H), 2.49-2.59 (m, 2H) 473 N-{4-[1-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) fluorobenzoyl)-1,2,3,6- ppm 8.11-8.13 (bs, 1H), 7.84-7.87 (m, 2H), m/e 442 tetrahydropyridin-4- 7.48 (td, J = 7.1, 1.8 Hz, 1H), 7.35-7.38 (m, 2H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.29-7.34 (m, 1H), 7.20-7.23 (m, 2H), 7.16-7.19 (m, 2H-isoindole-2- 2H), 7.14-7.17 (m, 1H), 7.10-7.12 (m, 1H), carboxamide 5.89-6.09 (m, 1H), 4.86 (s, 4H), 4.12-4.67 (m, 2H), 3.28-3.76 (m, 2H), 2.39-2.56 (m, 2H) 474 N-{4-[1-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) fluorobenzoyl)-1,2,3,6- ppm 8.12-8.14 (bs, 1H), 7.85-7.87 (m, 2H), m/e 442 tetrahydropyridin-4- 7.37-7.40 (m, 2H), 7.29-7.36 (m, 3H), 7.20-7.24 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.16-7.19 (m, 2H), 7.09-7.13 (m, 1H), 2H-isoindole-2- 5.97-6.00 (bs, 1H), 4.86 (s, 4H), 4.22-4.26 (m, 2H), carboxamide 3.68-3.73 (m, 2H), 2.49-2.53 (m, 2H) 475 N-{4-[1-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) fluorobenzoyl)-1,2,3,6- ppm 8.12-8.14 (bs, 1H), 7.85-7.87 (m, 2H), m/e 442 tetrahydropyridin-4- 7.53-7.58 (m, 2H), 7.38-7.41 (m, 2H), 7.20-7.25 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.16-7.20 (m, 2H), 7.09-7.14 (m, 2H), 2H-isoindole-2- 5.98-6.01 (m, 1H), 4.86 (s, 4H), 4.24-4.26 (m, 2H), carboxamide 3.70-3.74 (m, 2H), 2.50-2.55 (m, 2H) 476 N-{4-[1-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) chlorobenzoyl)-1,2,3,6- ppm 8.12-8.14 (bs, 1H), 7.85-7.87 (m, 2H), m/e 458 tetrahydropyridin-4- 7.46-7.50 (m, 2H), 7.38-7.40 (m, 4H), 7.20-7.25 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.15-7.19 (m, 2H), 5.98-6.01 (m, 1H), 4.86 (s, 2H-isoindole-2- 4H), 4.22-4.25 (m, 2H), 3.68-3.72 (m, 2H), carboxamide 2.50-2.54 (m, 2H) 477 N-(4-{1-[3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) (dimethylamino)benzoyl]- ppm 8.08-8.15 (m, 1H), 7.84-7.86 (m, 2H), m/e 467 1,2,3,6- 7.38-7.40 (m, 2H), 7.28 (dd, J = 8.2, 7.5 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.20-7.24 (m, 2H), 7.15-7.20 (m, 2H), 6.98-6.99 (m, yl}phenyl)-1,3-dihydro- 1H), 6.90-6.94 (m, 1H), 6.77-6.80 (m, 1H), 2H-isoindole-2- 5.99-6.02 (bs, 1H), 4.86 (s, 4H), 4.29-4.34 (m, 2H), carboxamide 3.71-3.83 (m, 2H), 2.79 (s, 6H), 2.51-2.54 (m, 2H) 478 N-(4-{1-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) (dimethylamino)benzoyl]- ppm 8.11 (d, J = 2.1 Hz, 1H), 7.84-7.87 (m, 2H), m/e 467 1,2,3,6- 7.56-7.59 (m, 2H), 7.39-7.41 (m, 2H), (M + H)⁺ tetrahydropyridin-4- 7.20-7.25 (m, 2H), 7.15-7.18 (m, 2H), 6.70-6.73 (m, 2H), yl}phenyl)-1,3-dihydro- 6.00-6.03 (m, 1H), 4.82-4.91 (m, 4H), 4.34 (q, J = 2.9 Hz, 2H-isoindole-2- 2H), 3.82 (t, J = 5.7 Hz, 2H), 2.82 (s, 6H), carboxamide 2.53-2.60 (m, 2H) 479 N-{4-[1-(3-furoyl)- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ (ESI(+)) 1,2,3,6-tetrahydropyridin- ppm 2.55 (d, J = 1.83 Hz, 2H), 3.77 (t, J = 5.80 Hz, 2 m/e 414 4-yl]phenyl}-1,3- H) 4.23 (q, J = 2.64 Hz, 2H), 4.77 (s, 4H), 6.08 (t, (M + H)⁺ dihydro-2H-isoindole-2- J = 3.51 Hz, 1H), 6.68 (d, J = 1.22 Hz, 1H), carboxamide 7.27-7.37 (m, 6H), 7.54 (d, J = 8.54 Hz, 2H), 7.67 (t, J = 1.68 Hz, 1H), 7.99 (s, 1H), 8.13 (s, 1H) 480 N-{4-[1-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) thienylcarbonyl)-1,2,3,6- ppm 8.11-8.12 (bs, 1H), 7.84-7.87 (m, 2H), m/e 430 tetrahydropyridin-4- 7.72-7.73 (m, 1H), 7.35-7.42 (m, 4H), 7.21-7.24 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.17-7.19 (m, 2H), 5.97-5.99 (bs, 1H), 2H-isoindole-2- 4.82-4.89 (m, 4H), 4.29-4.31 (m, 2H), 3.78 (t, J = 5.6 Hz, carboxamide 2H), 2.49-2.53 (m, 2H) 481 N-{4-[1-(1H-pyrrol-2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 11.78-11.92 (m, 1H), 8.09-8.11 (m, 1H), m/e 413 tetrahydropyridin-4- 7.83-7.86 (m, 2H), 7.37-7.40 (m, 2H), 7.20-7.23 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.16-7.20 (m, 2H), 7.08-7.10 (m, 1H), 2H-isoindole-2- 6.72-6.74 (m, 1H), 6.35 (dt, J = 3.6, 2.5 Hz, 1H), carboxamide 5.99-6.02 (m, 1H), 4.86 (s, 4H), 4.46 (q, J = 2.9 Hz, 2H), 3.98 (t, J = 5.7 Hz, 2H), 2.50-2.60 (m, 2H) 482 N-(4-{1-[(2,5-dimethyl- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) 1H-pyrrol-3-yl)carbonyl]- ppm 10.78-10.83 (m, 1H), 8.06-8.14 (m, 1H), m/e 441 1,2,3,6-tetrahydropyridin- 7.81-7.89 (m, 2H), 7.37-7.44 (m, 2H), 7.20-7.23 (m, (M + H)⁺ 4-yl}phenyl)-1,3- 2H), 7.16-7.19 (m, 2H), 6.11 (dd, J = 2.7, 1.2 Hz, dihydro-2H-isoindole-2- 1H), 6.04-6.06 (m, 1H), 4.82-4.91 (m, 4H), carboxamide 4.41-4.45 (m, 2H), 3.94 (t, J = 5.7 Hz, 2H), 2.54-2.61 (m, 2H), 2.48 (s, 3H), 2.24 (s, 3H) 483 N-{4-[1-(1,3-thiazol-4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.97 (d, J = 2.1 Hz, 1H), 8.16 (d, J = 2.1 Hz, m/e 431 tetrahydropyridin-4- 1H), 8.09-8.14 (m, 1H), 7.83-7.86 (m, 2H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.37-7.40 (m, 2H), 7.20-7.24 (m, 2H), 7.16-7.19 (m, 2H-isoindole-2- 2H), 6.01 (t, J = 3.2 Hz, 1H), 4.86 (s, 4H), carboxamide 4.48-4.51 (m, 2H), 3.98-4.01 (m, 2H), 2.56-2.62 (m, 2H) 484 N-{4-[1-(1H-pyrazol-4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.19-8.23 (m, 2H), 8.06-8.15 (m, 1H), m/e 414 tetrahydropyridin-4- 7.82-7.90 (m, 2H), 7.36-7.42 (m, 2H), 7.19-7.24 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.16-7.19 (m, 2H), 6.00-6.05 (m, 1H), 2H-isoindole-2- 4.83-4.89 (m, 4H), 4.40-4.44 (m, 2H), 3.92 (t, J = 5.7 Hz, carboxamide 2H), 2.52-2.59 (m, 2H) 485 N-(4-{1-[(3,5-dimethyl- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(−)) m/e 1,2-oxazol-4- ppm 8.14-8.16 (bs, 1H), 7.85-7.88 (m, 2H), 441 (M − H)⁻ yl)carbonyl]-1,2,3,6- 7.38-7.42 (m, 2H), 7.20-7.24 (m, 2H), 7.16-7.19 (m, tetrahydropyridin-4- 2H), 6.00-6.02 (m, 1H), 4.84-4.88 (m, 4H), yl}phenyl)-1,3-dihydro- 4.19-4.23 (m, 2H), 3.69-3.75 (m, 2H), 2.49-2.58 (m, 2H-isoindole-2- 2H), 2.32 (s, 3H), 2.29 (s, 3H) carboxamide 486 N-{4-[1-(pyridin-2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.61 (ddd, J = 4.8, 1.7, 0.9 Hz, 1H), m/e 425 tetrahydropyridin-4- 8.10-8.11 (bs, 1H), 7.83-7.86 (m, 2H), 7.76 (dt, J = 7.7, 1.1 Hz, (M + H)⁺ yl]phenyl}-1,3-dihydro- 1H), 7.68 (td, J = 7.6, 1.8 Hz, 1H), 2H-isoindole-2- 7.36-7.39 (m, 2H), 7.20-7.24 (m, 3H), 7.16-7.19 (m, 2H), carboxamide 5.89-6.10 (m, 1H), 4.86 (s, 4H), 4.40-4.42 (m, 2H), 3.56-4.22 (m, 2H), 2.52-2.64 (m, 2H) 487 N-{4-[1-(pyridin-3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.93 (d, J = 2.2 Hz, 1H), 8.70 (dd, J = 4.8, 1.7 Hz, m/e 425 tetrahydropyridin-4- 1H), 8.13-8.15 (bs, 1H), 7.85-7.88 (m, 2H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.80-7.85 (m, 1H), 7.37-7.40 (m, 2H), 2H-isoindole-2- 7.25-7.29 (m, 1H), 7.20-7.24 (m, 2H), 7.16-7.20 (m, 2H), carboxamide 5.97-5.99 (bs, 1H), 4.86 (s, 4H), 4.22-4.29 (m, 2H), 3.64-3.78 (m, 2H), 2.47-2.56 (m, 2H) 488 N-[4-(1-isonicotinoyl- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) 1,2,3,6-tetrahydropyridin- ppm 8.74-8.76 (m, 2H), 8.14-8.15 (bs, 1H), m/e 425 4-yl)phenyl]-1,3-dihydro- 7.85-7.88 (m, 2H), 7.36-7.42 (m, 4H), 7.20-7.24 (m, (M + H)⁺ 2H-isoindole-2- 2H), 7.16-7.19 (m, 2H), 5.97-6.00 (bs, 1H), 4.86 (s, carboxamide 4H), 4.13-4.32 (m, 2H), 3.57-3.79 (m, 2H), 2.46-2.55 (m, 2H) 489 N-{4-[1-(pyridazin-3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 9.22 (dd, J = 5.0, 1.8 Hz, 1H), 8.10-8.12 (bs, m/e 426 tetrahydropyridin-4- 1H), 7.90 (dd, J = 8.3, 1.7 Hz, 1H), 7.83-7.86 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 7.47-7.50 (m, 1H), 7.34-7.38 (m, 2H), 2H-isoindole-2- 7.20-7.23 (m, 2H), 7.16-7.20 (m, 2H), 5.92-6.05 (m, carboxamide 1H), 4.86 (s, 4H), 4.36-4.51 (m, 2H), 3.67-3.94 (m, 2H), 2.53-2.64 (m, 2H) 490 N-{4-[1-(pyrazin-2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 9.34 (d, J = 1.2 Hz, 1H), 8.86 (d, J = 4.9 Hz, m/e 426 tetrahydropyridin-4- 1H), 8.12-8.14 (bs, 1H), 7.84-7.87 (m, 2H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.69 (dd, J = 5.0, 1.5 Hz, 1H), 7.37-7.39 (m, 2H), 2H-isoindole-2- 7.20-7.23 (m, 2H), 7.16-7.19 (m, 2H), 5.92-6.05 (m, carboxamide 1H), 4.86 (s, 4H), 4.29-4.45 (m, 2H), 3.62-4.00 (m, 2H), 2.53-2.61 (m, 2H) 491 N-{4-[1-(pyrimidin-4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 9.13 (d, J = 1.5 Hz, 1H), 8.59 (d, J = 2.5 Hz, m/e 426 tetrahydropyridin-4- 1H), 8.51 (dd, J = 2.5, 1.3 Hz, 1H), 8.11-8.13 (bs, (M + H)⁺ yl]phenyl}-1,3-dihydro- 1H), 7.84-7.87 (m, 2H), 7.37-7.40 (m, 2H), 2H-isoindole-2- 7.20-7.24 (m, 2H), 7.16-7.19 (m, 2H), 5.95-6.05 (m, carboxamide 1H), 4.86 (s, 4H), 4.32-4.47 (m, 2H), 3.60-3.91 (m, 2H), 2.55-2.61 (m, 2H) 492 N-(4-{1-[3-(piperidin-1- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) yl)propanoyl]-1,2,3,6- ppm 8.12-8.13 (bs, 1H), 7.84-7.86 (m, 2H), m/e 459 tetrahydropyridin-4- 7.35-7.38 (m, 2H), 7.21-7.25 (m, 2H), 7.16-7.20 (m, (M + H)⁺ yl}phenyl)-1,3-dihydro- 2H), 5.94-5.98 (m, 1H), 4.84-4.89 (m, 4H), 2H-isoindole-2- 4.06-4.29 (m, 2H), 3.53-3.89 (m, 2H), 3.30 (t, J = 7.2 Hz, carboxamide 2H), 2.95-3.05 (m, 2H), 2.89-2.92 (m, 4H), 2.42-2.48 (m, 2H), 1.65-1.73 (m, 4H), 1.30-1.40 (m, 2H) 493 N-{4-[1-(morpholin-4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) ylacetyl)-1,2,3,6- ppm 8.13-8.14 (bs, 1H), 7.85-7.88 (m, 2H), m/e 447 tetrahydropyridin-4- 7.39-7.41 (m, 2H), 7.20-7.24 (m, 2H), 7.16-7.20 (m, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H), 6.01-6.04 (m, 1H), 4.86-4.87 (m, 4H), 4.27 (q, 2H-isoindole-2- J = 2.9 Hz, 2H), 3.75-3.80 (m, 2H), 3.64-3.72 (m, carboxamide 4H), 3.29 (s, 2H), 2.54-2.57 (m, 6H) 494 N-(4-{1-[(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ (ESI(+)) methylpiperazin-1- ppm 8.13-8.15 (bs, 1H), 7.85-7.87 (m, 2H), m/e 460 yl)acetyl]-1,2,3,6- 7.38-7.41 (m, 2H), 7.20-7.25 (m, 2H), 7.19 (d, J = 7.0 Hz, (M + H)⁺ tetrahydropyridin-4- 1H), 7.17-7.19 (m, 1H), 6.00-6.02 (m, 1H), yl}phenyl)-1,3-dihydro- 4.83-4.89 (m, 4H), 4.24-4.26 (m, 2H), 2H-isoindole-2- 3.74-3.77 (m, 2H), 3.33 (s, 2H), 2.73-2.76 (m, 4H), carboxamide 2.66-2.69 (m, 4H), 2.49-2.54 (m, 2H), 2.36 (s, 3H) 759 N-{4-[1-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-4-ylcarbonyl)- ppm 8.13 (s, 1H), 7.54 (m, 2H), 7.38-7.23 (m, m/e 432 1,2,3,6-tetrahydropyridin- 6H), 6.08 (m, 1H), 4.79 (d, J = 13.1 Hz, 4H), (M + H)⁺ 4-yl]phenyl}-1,3- 4.15 (m, 2H), 3.86 (m, 2H), 3.70 (t, J = 5.7 Hz, 2H), dihydro-2H-isoindole-2- 3.43 (td, J = 11.4, 2.4 Hz, 2H), 2.90 (m, 1H), carboxamide 2.50 (m, 2H), 1.76-1.51 (m, 4H) 760 N-{4-[1-(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.13 (s, 1H), 7.55 (m, 2H), 7.38-7.26 (m, m/e 434 tetrahydropyridin-4- 6H), 6.07 (m, 1H), 4.79 (m, 4H), 4.37 (dd, J = 9.2, (M + H)⁺ yl]phenyl}-1,3-dihydro- 3.0 Hz, 1H), 4.15 (m, 2H), 3.82-3.62 (m, 7H), 2H-isoindole-2- 3.53 (m, 1H), 2.50 (m, 2H) carboxamide 761 N-(4-{1-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpyrrolidin-3- ppm 8.13 (s, 1H), 7.54 (d, J = 8.6 Hz, 2H), m/e 431 yl)carbonyl]-1,2,3,6- 7.40-7.20 (m, 6H), 6.07 (s, 1H), 4.78 (s, 4H), 4.12 (m, (M + H)⁺ tetrahydropyridin-4- 2H), 3.68 (t, J = 5.7 Hz, 2H), 3.27 (m, 1H), yl}phenyl)-1,3-dihydro- 2.77 (m, 1H), 2.63-2.45 (m, 4H), 2.38 (m, 1H), 2.25 (s, 2H-isoindole-2- 3H), 98 (m, 2H) carboxamide 762 N-(4-{1-[(1,1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dioxidotetrahydrothiophen- ppm 8.14 (s, 1H), 7.55 (m, 2H), 7.38-7.27 (m, m/e 466 3-yl)carbonyl]-1,2,3,6- 6H), 6.08 (m, 1H), 4.81 (m, 4H), 4.17 (m, 2H), (M + H)⁺ tetrahydropyridin-4- 3.74 (m, 3H), 3.33-3.10 (m, 3H), 3.07 (m, 1H), yl}phenyl)-1,3-dihydro- 2.53 (m, 2H), 2.37 (m, 1H), 2.14 (m, 1H) 2H-isoindole-2- carboxamide 763 N-{4-[1-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpropanoyl)- ppm 8.13 (s, 1H), 7.54 (m, 2H), 7.38-7.27 (m, m/e 406 1,2,3,6-tetrahydropyridin- 6H), 6.09 (m, 1H), 5.10 (s, 1H), 4.78 (s, 4H), (M + H)⁺ 4-yl]phenyl}-1,3- 4.28 (m, 2H), 3.94 (m, 2H), 2.50 (m, 2H), 1.37 (s, 6H) dihydro-2H-isoindole-2- carboxamide 1019 5-cyano-N-{4-[1-(2- -¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpropanoyl)- ppm 8.20 (m, 1H), 7.80 (m, 1H), 7.70 (m, 1H), m/e 415 1,2,3,6-tetrahydropyridin- 7.54 (m, 3H), 7.37 (m, 2H), 6.08 (bs, 1H), 4.90 (m, 4H), (M + H)⁺ 4-yl]phenyl}-1,3- 4.13 (m, 2H), 3.69 (m, 2H), 2.90 (m, 1H), 2.50 (m, dihydro-2H-isoindole-2- 2H), 1.02 (m, 6H) carboxamide 1281 5-cyano-N-{4-[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (tetrahydrofuran-3- ppm 8.21 (s, 1H), 7.80 (s, 1H), 7.71 (d, J = 7.9 Hz, m/e 443 ylcarbonyl)-1,2,3,6- 1H), 7.54 (m, 3H), 7.33 (m, 2H), 6.07 (bs, 1H), (M + H)⁺ tetrahydropyridin-4- 4.83 (m, 4H), 4.14 (m, 2H), 3.91 (t, J = 8.1 Hz, yl]phenyl}-1,3-dihydro- 1H), 3.71 (m, 5H), 3.38 (m, 1H), 2.50 (m, 2H), 2H-isoindole-2- 2.07 (m, 2H) carboxamide 1282 5-cyano-N-{4-[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (tetrahydro-2H-pyran-4- ppm 8.22 (bs, 1H), 7.80 (s, 1H), 7.72 (d, J = 7.8 Hz, m/e 457 ylcarbonyl)-1,2,3,6- 1H), 7.54 (m, 3H), 7.33 (m, 2H), 6.08 (bs, 1H), (M + H)⁺ tetrahydropyridin-4- 4.82 (m, 4H), 4.14 (m, 2H), 3.86 (m, 2H), 3.70 (t, J = 5.7 Hz, yl]phenyl}-1,3-dihydro- 2H), 3.42 (td, J = 11.4, 2.5 Hz, 2H), 2H-isoindole-2- 2.90 (m, 1H), 2.50 (m, 2H), 1.77-1.53 (m, 4H) carboxamide 1283 5-cyano-N-{4-[1-(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) hydroxy-2- ppm 8.21 (s, 1H), 7.80 (s, 1H), 7.71 (d, J = 7.7 Hz, m/e 431 methylpropanoyl)- 1H), 7.53 (m, 3H), 7.33 (m, 2H), 6.08 (m, 1H), (M + H)⁺ 1,2,3,6-tetrahydropyridin- 5.10 (s, 1H), 4.83 (m, 4H), 4.28 (m, 2H), 3.93 (m, 2H), 4-yl]phenyl}-1,3- 2.50 (m, 2H), 1.37 (s, 6H) dihydro-2H-isoindole-2- carboxamide 1284 5-cyano-N-{4-[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (morpholin-4-ylacetyl)- ppm 8.21 (s, 1H), 7.80 (s, 1H), 7.72 (d, J = 7.9 Hz, m/e 472 1,2,3,6-tetrahydropyridin- 1H), 7.51 (m, 3H), 7.33 (m, 2H), 6.07 (m, 1H), (M + H)⁺ 4-yl]phenyl}-1,3- 4.83 (m, 4H), 4.15 (m, 2H), 3.71 (m, 2H), 3.58 (m, 4H), dihydro-2H-isoindole-2- 3.21 (s, 2H), 2.50 (m, 2H), 2.45 (m, 4H) carboxamide

Example 495 N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(5-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-2-yl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and benzoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.51 (bs, 1H), 8.32 (d, J=2.5 Hz, 1H), 7.90 (d, J=8.7 Hz, 1H), 7.77 (dd, J=8.7, 2.5 Hz, 1H), 7.48-7.39 (m, 5H), 7.36-7.25 (m, 4H), 6.16 (bs, 1H), 4.81 (s, 4H), 4.18 (m, 2H), 3.68 (m, 2H), 2.55 (m, 2H); MS (ESI(+)) m/e 425 (M+H)⁺.

Example 496 N-(4-{[6-(benzoylamino)hexyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-{4-[(6-aminohexyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.57 (s, 1H), 8.43 (t, J=5.6 Hz, 1H), 8.25 (t, J=5.6 Hz, 1H), 7.81-7.86 (m, 2H), 7.74-7.78 (m, 2H), 7.63-7.67 (m, 2H), 7.41-7.54 (m, 3H), 7.29-7.39 (m, 4H), 4.78-4.79 (bs, 4H), 3.15-3.27 (m, 4H), 1.44-1.64 (m, 4H), 1.19-1.39 (m, 4H); MS (ESI(+)) m/e 485 (M+H)⁺.

Example 497 N-[4-({4-[(benzoylamino)methyl]benzyl}carbamoyl)phenyl]-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(4-{[4-(aminomethyl)benzyl]carbamoyl}phenyl)-5-fluoro-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.01 (t, J=6.0 Hz, 1H), 8.83 (t, J=5.9 Hz, 1H), 8.60 (s, 1H), 7.85-7.91 (m, 2H), 7.78-7.83 (m, 2H), 7.63-7.68 (m, 2H), 7.36-7.56 (m, 4H), 7.27 (s, 4H), 7.21-7.26 (m, 1H), 7.10-7.19 (m, 1H), 4.72-4.81 (m, 4H), 4.40-4.48 (m, 4H); MS (ESI(+)) m/e 523 (M+H)⁺.

TABLE 8 The following Examples were essentially prepared as described in Example 1C, substituting N-(4-(piperazin-1-yl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1- amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 498 N-{4-[4-(5-oxo-L- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) prolyl)piperazin-1- 7.95-7.98 (bs, 1H), 7.81-7.90 (m, 1H), 7.74-7.77 (m, m/e 434 yl]phenyl}-1,3- 2H), 7.20-7.23 (m, 2H), 7.16-7.20 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 6.92-6.95 (m, 2H), 4.86 (s, 4H), 4.60-4.64 (m, 1H), 2-carboxamide 3.55-3.76 (m, 4H), 3.03-3.06 (m, 4H), 2.38-2.47 (m, 1H), 2.25-2.37 (m, 2H), 2.08-2.15 (m, 1H) 499 N-{4-[4-(5-oxo-D- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) prolyl)piperazin-1- 7.95-7.98 (bs, 1H), 7.80-7.84 (bs, 1H), 7.75-7.77 (m, m/e 434 yl]phenyl}-1,3- 2H), 7.20-7.23 (m, 2H), 7.16-7.20 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 6.92-6.95 (m, 2H), 4.86 (s, 4H), 4.60-4.64 (m, 1H), 2-carboxamide 3.57-3.76 (m, 4H), 3.02-3.08 (m, 4H), 2.38-2.46 (m, 1H), 2.24-2.37 (m, 2H), 2.08-2.15 (m, 1H) 500 N-(4-{4-[(1- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) acetylpiperidin-4- 7.93-7.95 (bs, 1H), 7.75-7.77 (m, 2H), 7.20-7.23 (m, m/e 476 yl)carbonyl]piperazin- 2H), 7.19 (d, J = 4.2 Hz, 1H), 7.16 (d, J = 8.2 Hz, (M + H)⁺ 1-yl}phenyl)-1,3- 1H), 6.94-6.97 (m, 2H), 4.86 (s, 4H), 3.66-3.76 (m, dihydro-2H-isoindole- 4H), 3.05-3.08 (m, 4H), 2.78-3.03 (m, 3H), 2.01 (s, 2-carboxamide 3H), 1.81-1.92 (m, 2H), 1.68-1.79 (m, 2H) 501 N-{4-[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) acetamidobenzoyl)piperazin- 9.65 (d, J = 5.2 Hz, 1H), 8.26 (d, J = 8.1 Hz, 1H), m/e 484 1-yl]phenyl}- 7.92-7.93 (bs, 1H), 7.73-7.76 (m, 2H), 7.34-7.39 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 7.20-7.23 (m, 2H), 7.16-7.19 (m, 2H), 7.12 (dd, isoindole-2- J = 7.5, 1.2 Hz, 1H), 6.92-6.94 (m, 2H), 4.86 (s, 4H), carboxamide 3.68-3.83 (m, 4H), 3.07-3.10 (m, 4H), 2.09 (s, 3H) 502 N-(4-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (methylsulfonyl)benzoyl]piperazin- 8.10-8.13 (m, 2H), 7.94-7.96 (bs, 1H), 7.75-7.78 (m, m/e 505 1- 2H), 7.68-7.71 (m, 2H), 7.20-7.23 (m, 2H), (M + H)⁺ yl}phenyl)-1,3- 7.16-7.20 (m, 2H), 6.94-6.98 (m, 2H), 4.86 (s, 4H), dihydro-2H-isoindole- 3.55-3.78 (m, 4H), 3.17 (s, 3H), 3.08-3.11 (m, 4H) 2-carboxamide 503 N-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) butyrylpiperazin-1- 7.91-7.93 (m, 1H), 7.73-7.77 (m, 2H), 7.20-7.23 (m, m/e 393 yl)phenyl]-1,3- 2H), 7.19 (d, J = 7.3 Hz, 1H), 7.17-7.18 (m, 1H), (M + H)⁺ dihydro-2H-isoindole- 6.93-6.96 (m, 2H), 4.86 (s, 4H), 3.48-3.70 (m, 3H), 2-carboxamide 3.02-3.06 (m, 4H), 2.43 (d, J = 0.6 Hz, 1H), 2.31 (t, J = 7.3 Hz, 2H), 1.65-1.81 (m, 2H), 0.95 (t, J = 7.3 Hz, 3H) 504 N-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) isobutyrylpiperazin-1- 7.92-7.94 (bs, 1H), 7.74-7.76 (m, 2H), 7.20-7.23 (m, m/e 393 yl)phenyl]-1,3- 2H), 7.16-7.20 (m, 2H), 6.93-6.96 (m, 2H), 4.86 (s, (M + H)⁺ dihydro-2H-isoindole- 4H), 3.65-3.69 (m, 4H), 3.03-3.06 (m, 4H), 2-carboxamide 2.76-2.87 (m, 1H), 1.15 (d, J = 6.7 Hz, 6H) 505 N-{4-[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) methylbutanoyl)piperazin- 7.92-7.94 (bs, 1H), 7.74-7.77 (m, 2H), 7.20-7.23 (m, m/e 407 1-yl]phenyl}-1,3- 2H), 7.16-7.20 (m, 2H), 6.94-6.97 (m, 2H), 4.86 (s, (M + H)⁺ dihydro-2H-isoindole- 4H), 3.68-3.73 (m, 4H), 3.04-3.07 (m, 4H), 2.68 (h, J = 6.7 Hz, 2-carboxamide 1H), 1.76-1.87 (m, 1H), 1.40-1.51 (m, 1H), 1.15 (d, J = 6.7 Hz, 3H), 0.91 (t, J = 7.4 Hz, 3H) 506 N-{4-[4-(3,3,3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) trifluoropropanoyl)piperazin- 7.93-7.95 (bs, 1H), 7.74-7.76 (m, 2H), 7.20-7.24 (m, m/e 433 1-yl]phenyl}- 2H), 7.16-7.19 (m, 2H), 6.92-6.95 (m, 2H), 4.86 (s, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.58-3.78 (m, 4H), 3.57 (q, J = 10.5 Hz, 2H), isoindole-2- 3.02-3.09 (m, 4H) carboxamide 507 N-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (methoxyacetyl)piperazin- 7.92-7.96 (bs, 1H), 7.73-7.76 (m, 2H), 7.16-7.24 (m, m/e 395 1-yl]phenyl}-1,3- 4H), 6.92-6.95 (m, 2H), 4.86 (s, 4H), 4.18 (s, 2H), (M + H)⁺ dihydro-2H-isoindole- 3.55-3.78 (m, 4H), 3.39 (s, 3H), 3.03-3.06 (m, 4H) 2-carboxamide 508 N-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (tetrahydrofuran-2- 7.90-7.95 (m, 1H), 7.73-7.75 (m, 2H), 7.19-7.24 (m, m/e 421 ylcarbonyl)piperazin- 2H), 7.15-7.19 (m, 2H), 6.92-6.95 (m, 2H), 4.86 (s, (M + H)⁺ 1-yl]phenyl}-1,3- 4H), 4.66 (dd, J = 7.2, 5.4 Hz, 1H), 3.88-3.94 (m, dihydro-2H-isoindole- 1H), 3.67-3.83 (m, 5H), 2.93-3.15 (m, 4H), 2-carboxamide 2.37-2.48 (m, 1H), 1.84-2.05 (m, 2H), 1.70-1.81 (m, 1H) 509 N-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (tetrahydrofuran-3- 7.93 (d, J = 2.6 Hz, 1H), 7.74-7.77 (m, 2H), m/e 421 ylcarbonyl)piperazin- 7.20-7.24 (m, 2H), 7.15-7.20 (m, 2H), 6.94-6.97 (m, 2H), (M + H)⁺ 1-yl]phenyl}-1,3- 4.86 (s, 4H), 4.08 (dd, J = 8.3, 6.5 Hz, 1H), 4.04 (t, J = 8.0 Hz, dihydro-2H-isoindole- 1H), 3.91 (td, J = 7.9, 5.9 Hz, 1H), 3.74-3.82 (m, 2-carboxamide 1H), 3.58-3.76 (m, 4H), 3.26-3.34 (m, 1H), 3.00-3.10 (m, 4H), 2.24-2.33 (m, 1H), 1.97-2.07 (m, 1H) 510 N-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (cyclopentylacetyl)piperazin- 7.90-7.92 (bs, 1H), 7.73-7.76 (m, 2H), 7.19-7.24 (m, m/e 433 1-yl]phenyl}- 2H), 7.15-7.19 (m, 2H), 6.94-6.97 (m, 2H), 4.85 (s, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.46-3.83 (m, 4H), 3.04-3.07 (m, 4H), isoindole-2- 2.28-2.49 (m, 3H), 1.81-1.96 (m, 2H), 1.41-1.67 (m, 4H), carboxamide 1.17-1.32 (m, 2H) 511 N-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (cyclohexylcarbonyl)piperazin- 7.90-7.92 (bs, 1H), 7.73-7.76 (m, 2H), 7.20-7.24 (m, m/e 433 1-yl]phenyl}- 2H), 7.15-7.20 (m, 2H), 6.94-6.97 (m, 2H), 4.86 (s, (M + H)⁺ 1,3-dihydro-2H- 4H), 3.64-3.77 (m, 4H), 3.04-3.07 (m, 4H), 2.60 (tt, J = 11.0, isoindole-2- 3.5 Hz, 1H), 1.55-1.85 (m, 7H), 1.14-1.40 (m, carboxamide 3H) 512 N-{4-[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) methoxybenzoyl)piperazin- 7.90-7.92 (bs, 1H), 7.73-7.76 (m, 2H), 7.41 (dd, J = 7.4, m/e 457 1-yl]phenyl}-1,3- 1.8 Hz, 1H), 7.30-7.35 (m, 1H), 7.19-7.24 (m, (M + H)⁺ dihydro-2H-isoindole- 2H), 7.15-7.19 (m, 2H), 7.01 (td, J = 7.4, 1.0 Hz, 1H), 2-carboxamide 6.92-6.98 (m, 3H), 4.85 (s, 4H), 3.77-4.30 (m, 2H), 3.70 (s, 3H), 3.51 (s, 2H), 2.79-3.24 (m, 4H) 513 N-{4-[4-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) methoxybenzoyl)piperazin- 7.92 (d, J = 2.1 Hz, 1H), 7.74-7.76 (m, 2H), m/e 457 1-yl]phenyl}-1,3- 7.30-7.34 (m, 1H), 7.19-7.24 (m, 3H), 7.15-7.19 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.11-7.14 (m, 1H), 7.01 (ddd, J = 8.2, 2.6, 1.0 Hz, 1H), 2-carboxamide 6.93-6.96 (m, 2H), 4.86 (s, 4H), 3.67-3.79 (m, 7H), 3.06-3.09 (m, 4H) 514 N-{4-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) methoxybenzoyl)piperazin- 7.89-7.92 (m, 1H), 7.74-7.76 (m, 2H), 7.53-7.56 (m, m/e 457 1-yl]phenyl}-1,3- 2H), 7.20-7.23 (m, 2H), 7.15-7.20 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 6.90-7.01 (m, 4H), 4.86 (s, 4H), 3.73-3.78 (m, 4H), 3.71 (s, 2-carboxamide 3H), 3.08-3.11 (m, 4H) 515 N-{4-[4-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) fluorobenzoyl)piperazin- 7.91-7.93 (bs, 1H), 7.74-7.77 (m, 2H), 7.29-7.41 (m, m/e 445 1-yl]phenyl}-1,3- 3H), 7.20-7.23 (m, 2H), 7.16-7.20 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.09-7.14 (m, 1H), 6.94-6.97 (m, 2H), 4.86 (s, 4H), 2-carboxamide 3.65-3.83 (m, 4H), 3.06-3.09 (m, 4H) 516 N-{4-[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) chlorobenzoyl)piperazin- 7.91-7.94 (bs, 1H), 7.74-7.76 (m, 2H), 7.34-7.45 (m, m/e 461 1-yl]phenyl}-1,3- 2H), 7.25-7.29 (m, 2H), 7.19-7.23 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.16-7.19 (m, 2H), 6.94-6.96 (m, 2H), 4.85 (s, 4H), 2-carboxamide 3.72-4.17 (m, 2H), 3.26-3.50 (m, 2H), 2.84-3.25 (m, 4H) 517 N-{4-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) chlorobenzoyl)piperazin- 7.91-7.93 (bs, 1H), 7.74-7.77 (m, 2H), 7.47-7.49 (m, m/e 461 1-yl]phenyl}-1,3- 2H), 7.38-7.41 (m, 2H), 7.20-7.23 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.16-7.19 (m, 2H), 6.94-6.97 (m, 2H), 4.86 (s, 4H), 2-carboxamide 3.68-3.71 (m, 4H), 3.07-3.10 (m, 4H) 518 N-{4-[4-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(−)) cyanobenzoyl)piperazin- 7.92-7.94 (bs, 1H), 7.88-7.89 (m, 1H), 7.75-7.77 (m, m/e 450 1-yl]phenyl}-1,3- 2H), 7.71 (dt, J = 7.7, 1.4 Hz, 1H), 7.65 (dt, J = 7.7, (M − H)⁻ dihydro-2H-isoindole- 1.4 Hz, 1H), 7.44 (t, J = 7.7 Hz, 1H), 7.20-7.23 (m, 2-carboxamide 2H), 7.16-7.20 (m, 2H), 6.94-6.97 (m, 2H), 4.86 (s, 4H), 3.57-3.83 (m, 4H), 3.08-3.11 (m, 4H) 519 N-{4-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) cyanobenzoyl)piperazin- 7.93-7.94 (bs, 1H), 7.74-7.77 (m, 2H), 7.65-7.71 (m, m/e 452 1-yl]phenyl}-1,3- 2H), 7.56-7.61 (m, 2H), 7.20-7.23 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.16-7.19 (m, 2H), 6.94-6.97 (m, 2H), 4.86 (s, 4H), 2-carboxamide 3.58-3.77 (m, 4H), 3.08-3.11 (m, 4H) 520 N-(4-{4-[3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (dimethylamino)benzoyl]piperazin- 7.91 (d, J = 2.6 Hz, 1H), 7.73-7.76 (m, 2H), m/e 470 1- 7.26-7.31 (m, 1H), 7.19-7.23 (m, 2H), 7.16-7.19 (m, 2H), (M + H)⁺ yl}phenyl)-1,3- 6.96-6.99 (m, 1H), 6.93-6.97 (m, 2H), 6.90 (dt, J = 7.3, 1.1 Hz, dihydro-2H-isoindole- 1H), 6.78 (ddd, J = 8.4, 2.7, 0.8 Hz, 1H), 4.85 (s, 2-carboxamide 4H), 3.71-3.83 (m, 4H), 3.07-3.10 (m, 4H), 2.80 (s, 6H) 521 N-(4-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) (dimethylamino)benzoyl]piperazin- 7.89-7.91 (bs, 1H), 7.73-7.76 (m, 2H), 7.55-7.57 (m, m/e 470 1- 2H), 7.19-7.23 (m, 2H), 7.16-7.19 (m, 2H), (M + H)⁺ yl}phenyl)-1,3- 6.94-6.97 (m, 2H), 6.71-6.73 (m, 2H), 4.86 (s, 4H), dihydro-2H-isoindole- 3.78-3.81 (m, 4H), 3.09-3.12 (m, 4H), 2.81-2.84 (m, 6H) 2-carboxamide 522 N-{4-[4-(3,4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) dimethoxybenzoyl)piperazin- 7.91-7.93 (bs, 1H), 7.74-7.77 (m, 2H), 7.26 (d, J = 2.0 Hz, m/e 487 1-yl]phenyl}- 1H), 7.20-7.24 (m, 2H), 7.16-7.19 (m, 3H), (M + H)⁺ 1,3-dihydro-2H- 6.93-7.00 (m, 3H), 4.86 (s, 4H), 3.77-3.80 (m, 4H), isoindole-2- 3.77 (s, 3H), 3.77 (s, 3H), 3.07-3.15 (m, 4H) carboxamide 523 N-{4-[4-(3,5- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) dimethoxybenzoyl)piperazin- 7.91-7.93 (bs, 1H), 7.74-7.76 (m, 2H), 7.20-7.24 (m, m/e 487 1-yl]phenyl}- 2H), 7.16-7.19 (m, 2H), 6.94-6.96 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 6.81-6.82 (m, 2H), 6.67 (t, J = 2.3 Hz, 1H), 4.86 (s, 4H), isoindole-2- 3.70-3.77 (m, 4H), 3.71 (s, 6H), 3.07-3.10 (m, 4H) carboxamide 524 N-(4-{4-[(3,4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) dimethoxyphenyl)acetyl]piperazin- 7.88-7.90 (bs, 1H), 7.71-7.74 (m, 2H), 7.19-7.23 (m, m/e 501 1- 2H), 7.15-7.19 (m, 2H), 7.09 (d, J = 2.0 Hz, 1H), (M + H)⁺ yl}phenyl)-1,3- 6.97 (dd, J = 8.1, 2.0 Hz, 1H), 6.88-6.93 (m, 3H), 4.85 (s, dihydro-2H-isoindole- 4H), 3.81 (s, 2H), 3.74 (s, 3H), 3.73 (s, 3H), 2-carboxamide 3.67-3.78 (m, 4H), 3.00-3.03 (m, 4H) 525 N-{4-[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) furoyl)piperazin-1- 7.89-7.91 (bs, 1H), 7.73-7.76 (m, 2H), 7.57 (dd, J = 1.8, m/e 417 yl]phenyl}-1,3- 0.9 Hz, 1H), 7.20-7.23 (m, 2H), 7.16-7.19 (m, (M + H)⁺ dihydro-2H-isoindole- 2H), 7.08 (dd, J = 3.4, 0.8 Hz, 1H), 6.93-6.96 (m, 2-carboxamide 2H), 6.45 (dd, J = 3.4, 1.7 Hz, 1H), 4.85 (s, 4H), 3.86-3.89 (m, 4H), 3.09-3.12 (m, 4H) 526 N-{4-[4-(3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) furoyl)piperazin-1- 7.93 (dd, J = 1.6, 0.8 Hz, 1H), 7.90-7.92 (bs, 1H), m/e 417 yl]phenyl}-1,3- 7.73-7.76 (m, 2H), 7.52-7.53 (m, 1H), 7.19-7.23 (m, (M + H)⁺ dihydro-2H-isoindole- 2H), 7.16-7.19 (m, 2H), 6.93-6.96 (m, 2H), 6.72 (dd, 2-carboxamide J = 1.8, 0.9 Hz, 1H), 4.85 (s, 4H), 3.77-3.80 (m, 4H), 3.06-3.10 (m, 4H) 527 N-{4-[4-(1H-pyrrol-2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(−)) ylcarbonyl)piperazin- 11.87-11.96 (bs, 1H), 7.88-7.89 (bs, 1H), m/e 414 1-yl]phenyl}-1,3- 7.72-7.75 (m, 2H), 7.19-7.23 (m, 2H), 7.15-7.19 (m, 2H), (M − H)⁻ dihydro-2H-isoindole- 7.10 (td, J = 2.7, 1.3 Hz, 1H), 6.92-6.95 (m, 2H), 2-carboxamide 6.68-6.70 (m, 1H), 6.33-6.36 (m, 1H), 4.85 (s, 4H), 3.94-3.97 (m, 4H), 3.09-3.12 (m, 4H) 528 N-{4-[4-(1H-pyrazol- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) 5- 7.88 (d, J = 2.5 Hz, 1H), 7.77 (d, J = 2.2 Hz, 1H), m/e 417 ylcarbonyl)piperazin- 7.71-7.74 (m, 2H), 7.19-7.23 (m, 2H), 7.15-7.19 (m, (M + H)⁺ 1-yl]phenyl}-1,3- 2H), 6.91-6.95 (m, 3H), 4.85 (s, 4H), 4.06-4.14 (m, dihydro-2H-isoindole- 4H), 3.07-3.18 (m, 4H) 2-carboxamide 529 N-{4-[4-(pyridin-2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) ylcarbonyl)piperazin- 8.60 (ddd, J = 4.8, 1.8, 0.9 Hz, 1H), 7.84-7.97 (m, m/e 428 1-yl]phenyl}-1,3- 1H), 7.76 (dt, J = 7.7, 1.1 Hz, 1H), 7.72-7.75 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.69 (td, J = 7.6, 1.8 Hz, 1H), 7.20-7.24 (m, 2H), 2-carboxamide 7.17-7.19 (m, 2H), 6.93-6.96 (m, 2H), 4.85 (s, 4H), 3.73-3.99 (m, 4H), 3.08-3.19 (m, 4H) 530 N-{4-[4-(pyridin-3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) ylcarbonyl)piperazin- 8.92 (dd, J = 2.2, 0.9 Hz, 1H), 8.70 (dd, J = 4.8, 1.7 Hz, m/e 428 1-yl]phenyl}-1,3- 1H), 7.90-8.02 (m, 1H), 7.82 (dt, J = 7.8, 2.0 Hz, (M + H)⁺ dihydro-2H-isoindole- 1H), 7.74-7.77 (m, 2H), 7.27 (ddd, J = 7.7, 4.8, 0.9 Hz, 2-carboxamide 1H), 7.20-7.23 (m, 2H), 7.16-7.19 (m, 2H), 6.93-6.96 (m, 2H), 4.86 (s, 4H), 3.68-3.72 (m, 4H), 3.06-3.09 (m, 4H) 531 N-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) isonicotinoylpiperazin- 8.74-8.76 (m, 2H), 7.95 (d, J = 2.8 Hz, 1H), m/e 428 1-yl)phenyl]-1,3- 7.75-7.78 (m, 2H), 7.38-7.40 (m, 2H), 7.20-7.23 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.16-7.20 (m, 2H), 6.94-6.97 (m, 2H), 4.86 (s, 4H), 2-carboxamide 3.56-3.76 (m, 4H), 3.06-3.09 (m, 4H) 532 N-{4-[4-(pyridazin-3- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) ylcarbonyl)piperazin- 9.22 (dd, J = 5.0, 1.7 Hz, 1H), 7.91 (dd, J = 8.3, 1.8 Hz, m/e 429 1-yl]phenyl}-1,3- 1H), 7.89-7.92 (bs, 1H), 7.72-7.75 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.51 (dd, J = 8.5, 5.1 Hz, 1H), 7.19-7.23 (m, 2H), 2-carboxamide 7.16-7.19 (m, 2H), 6.92-6.95 (m, 2H), 4.85 (s, 4H), 3.60-4.20 (m, 4H), 2.94-3.32 (m, 4H) 533 N-{4-[4-(pyrazin-2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) ylcarbonyl)piperazin- 9.33 (d, J = 1.4 Hz, 1H), 8.87 (d, J = 5.0 Hz, 1H), m/e 429 1-yl]phenyl}-1,3- 7.91-7.93 (bs, 1H), 7.73-7.76 (m, 2H), 7.70 (dd, J = 5.0, (M + H)⁺ dihydro-2H-isoindole- 1.4 Hz, 1H), 7.20-7.23 (m, 2H), 7.18 (t, J = 3.4 Hz, 2-carboxamide 2H), 6.94-6.96 (m, 2H), 4.85 (s, 4H), 3.48-4.06 (m, 4H), 3.12-3.15 (m, 4H) 534 N-{4-[4-(pyrimidin-4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) ylcarbonyl)piperazin- 9.13 (d, J = 1.5 Hz, 1H), 8.59 (d, J = 2.5 Hz, 1H), m/e 429 1-yl]phenyl}-1,3- 8.50 (dd, J = 2.5, 1.5 Hz, 1H), 7.91 (d, J = 0.8 Hz, (M + H)⁺ dihydro-2H-isoindole- 1H), 7.73-7.76 (m, 2H), 7.20-7.23 (m, 2H), 2-carboxamide 7.16-7.18 (m, 2H), 6.94-6.97 (m, 2H), 4.85 (s, 4H), 3.73-3.96 (m, 4H), 3.07-3.22 (m, 4H) 535 N-{4-[4-(N,N- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) dimethyl-beta- 7.90-7.93 (bs, 1H), 7.72-7.75 (m, 2H), 7.20-7.23 (m, m/e 422 alanyl)piperazin-1- 2H), 7.16-7.19 (m, 2H), 6.90-6.93 (m, 2H), 4.85 (s, (M + H)⁺ yl]phenyl}-1,3- 4H), 3.55-3.72 (m, 4H), 3.33 (t, J = 7.2 Hz, 2H), dihydro-2H-isoindole- 3.00-3.05 (m, 4H), 2.96 (t, J = 7.2 Hz, 2H), 2.64 (s, 2-carboxamide 6H) 536 N-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) acetylpiperazin-1- 7.89-7.92 (bs, 1H), 7.73-7.75 (m, 2H), 7.20-7.23 (m, m/e 365 yl)phenyl]-1,3- 2H), 7.15-7.19 (m, 2H), 6.92-6.95 (m, 2H), 4.85 (s, (M + H)⁺ dihydro-2H-isoindole- 4H), 3.48-3.81 (m, 4H), 2.97-3.03 (m, 4H), 2.04 (s, 2-carboxamide 3H) 537 N-{4-[4-(2- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) fluorobenzoyl)piperazin- 7.90-7.92 (bs, 1H), 7.73-7.76 (m, 2H), 7.46-7.51 (m, m/e 445 1-yl]phenyl}-1,3- 1H), 7.29-7.36 (m, 1H), 7.19-7.23 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.16-7.18 (m, 3H), 7.09-7.12 (m, 1H), 6.93-6.95 (m, 2H), 2-carboxamide 4.85 (s, 4H), 3.38-4.02 (m, 4H), 2.90-3.23 (m, 4H) 538 N-{4-[4-(4- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) fluorobenzoyl)piperazin- 7.91-7.93 (bs, 1H), 7.74-7.77 (m, 2H), 7.52-7.58 (m, m/e 445 1-yl]phenyl}-1,3- 2H), 7.20-7.25 (m, 2H), 7.16-7.20 (m, 2H), (M + H)⁺ dihydro-2H-isoindole- 7.09-7.15 (m, 2H), 6.94-6.97 (m, 2H), 4.86 (s, 4H), 2-carboxamide 3.69-3.72 (m, 4H), 3.07-3.10 (m, 4H) 539 N-{4-[4- ¹H NMR (400 MHz, Pyridine-d₅-D₂O, Temp = 90° C.) (ESI(+)) (phenylacetyl)piperazin- δ ppm 2.95-3.04 (m, 4H), 3.68 (s, 4H), 3.83 (s, 2 m/e 441 1-yl]phenyl}-1,3- H), 4.85 (s, 4H), 6.87-6.93 (m, 2H), 7.15-7.24 (m, (M + H)⁺ dihydro-2H-isoindole- 4H), 7.27-7.33 (m, 2H), 7.40 (d, J = 7.02 Hz, 2H), 2-carboxamide 7.68-7.75 (m, 2H), 7.89 (s, 1H) 540 N-{4-[4-(1,3-thiazol- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(−)) 4- 8.97 (d, J = 2.1 Hz, 1H), 8.17 (d, J = 2.1 Hz, 1H), m/e 432 ylcarbonyl)piperazin- 7.88-7.89 (bs, 1H), 7.72-7.75 (m, 2H), 7.19-7.23 (m, (M − H)⁻ 1-yl]phenyl}-1,3- 2H), 7.16-7.19 (m, 2H), 6.93-6.96 (m, 2H), 4.85 (s, dihydro-2H-isoindole- 4H), 3.98-4.01 (m, 4H), 3.13-3.16 (m, 4H) 2-carboxamide 541 N-{4-[4-(morpholin- ¹H NMR (400 MHz, Pyridine-d₅, Temp = 90° C.) δ ppm (ESI(+)) 4-ylacetyl)piperazin- 7.85-8.03 (m, 1H), 7.74-7.77 (m, 2H), 7.21-7.23 (m, m/e 450 1-yl]phenyl}-1,3- 2H), 7.16-7.19 (m, 2H), 6.97 (d, J = 7.0 Hz, 1H), (M + H)⁺ dihydro-2H-isoindole- 6.95-6.95 (m, 1H), 4.86 (s, 4H), 3.73-3.76 (m, 4H), 2-carboxamide 3.64-3.71 (m, 4H), 3.29 (s, 2H), 3.07-3.10 (m, 4H), 2.54-2.57 (m, 4H)

Example 542 5-cyano-N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 4-phenylbutyl isocyanate for methyl 4-isocyanatobenzoate and 5-cyanoisoindoline for isoindoline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.82 (s, 1H), 7.74 (dd, J=7.9, 1.5 Hz, 1H), 7.53 (d, J=7.9 Hz, 1H), 7.24-7.31 (m, 2H), 7.08-7.22 (m, 3H), 6.38 (t, J=5.6 Hz, 1H), 4.59-4.64 (m, 4H), 3.06-3.13 (m, 2H), 2.58 (t, J=7.5 Hz, 2H), 1.53-1.68 (m, 2H), 1.36-1.51 (m, 2H); MS (ESI(+)) m/e 319 (M+H)⁺.

Example 543 N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 543A N-(4-bromophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 1A, substituting 4-bromophenyl isocyanate for methyl 4-isocyanatobenzoate and 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine for isoindoline.

Example 543B tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 280, substituting tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide.

Example 543C N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 543D N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 278, substituting butyryl chloride for acetyl chloride and N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.46 (s, 1H), 7.54-7.57 (m, 2H), 7.43 (d, J=5.0 Hz, 1H), 7.32-7.39 (m, 2H), 6.09-6.11 (m, 1H), 4.79-4.82 (m, 4H), 4.08-4.14 (m, 2H), 3.58-3.68 (m, 2H), 2.39-2.55 (m, 2H), 2.34 (dt, J=19.9, 7.4 Hz, 2H), 1.47-1.62 (m, 2H), 0.88-0.93 (m, 3H); MS (ESI(+)) m/e 391 (M+H)⁺.

Example 544 N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 278, substituting isobutyryl chloride for acetyl chloride and N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.46 (s, 1H), 7.54-7.57 (m, 2H), 7.43 (d, J=5.1 Hz, 1H), 7.34-7.38 (m, 2H), 6.10-6.13 (bs, 1H), 4.79-4.82 (m, 4H), 4.07-4.21 (m, 2H), 3.67-3.70 (m, 2H), 2.85-3.01 (m, 1H), 2.39-2.55 (m, 2H), 0.97-1.08 (m, 6H); MS (ESI(+)) m/e 391 (M+H)⁺.

Example 545 N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.46 (s, 1H), 7.55-7.58 (m, 2H), 7.42-7.49 (m, 6H), 7.35-7.41 (m, 2H), 5.98-6.21 (m, 1H), 4.79-4.82 (m, 4H), 3.95-4.39 (m, 2H), 3.79-3.93 (m, 1H), 3.51-3.61 (m, 1H), 2.46-2.60 (m, 2H); MS (ESI(+)) m/e 425 (M+H)⁺.

TABLE 9 The following Examples were essentially prepared as described in Example 1C, substituting N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)- carboxamide for 3-phenylpropan-1-amine and the corresponding carboxylic acid for 4- (isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 546 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.61 (s, (ESI(+)) 3-ylcarbonyl)-1,2,3,6- 1H), 8.50 (d, J = 5.0 Hz, 1H), 8.46 (s, 1H), m/e 419 tetrahydropyridin-4- 7.54-7.57 (m, 2H), 7.43 (d, J = 5.0 Hz, 1H), 7.36 (dd, J = 8.4, (M + H)⁺ yl]phenyl}-1,3-dihydro- 4.2 Hz, 2H), 6.09-6.12 (m, 1H), 2H-pyrrolo[3,4- 4.75-4.87 (m, 4H), 4.10-4.21 (m, 2H), 3.90 (dt, J = 11.3, 8.1 Hz, c]pyridine-2-carboxamide 1H), 3.66-3.75 (m, 5H), 3.32-3.50 (m, 1H), 2.41-2.57 (m, 2H), 1.95-2.10 (m, 2H) 620 N-(4-{1-[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxyethoxy)acetyl]- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 437 1,2,3,6-tetrahydropyridin- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.0 Hz, 1H), (M + H)⁺ 4-yl}phenyl)-1,3- 7.32 (m, 2H), 6.06 (m, 1H), 4.80 (d, J = 8.9 Hz, 4H), dihydro-2H-pyrrolo[3,4- 4.18 (s, 2H), 4.10 (m, 2H), 3.65 (t, J = 5.7 Hz, c]pyridine-2-carboxamide 2H), 3.60 (m, 2H), 3.49 (m, 2H), 3.27 (s, 3H), 2.50 (m, 2H) 705 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 2-ylcarbonyl)-1,2,3,6- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 419 tetrahydropyridin-4- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.5 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.33 (m, 2H), 6.07 (m, 1H), 4.79 (m, 4H), 4.67 (dd, J = 7.6, 2H-pyrrolo[3,4- 5.6 Hz, 1H), 4.14 (bs, 2H), 3.85-3.64 (m, c]pyridine-2-carboxamide 4H), 2.50 (m, 2H), 2.11 (m, 1H), 2.00 (m, 1H), 1.85 (m, 2H) 706 N-{4-[1-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-4-ylcarbonyl)- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 433 1,2,3,6-tetrahydropyridin- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.2 Hz, 1H), (M + H)⁺ 4-yl]phenyl}-1,3- 7.33 (m, 2H), 6.07 (m, 1H), 4.80 (m, 4H), 4.14 (bs, dihydro-2H-pyrrolo[3,4- 2H), 3.86 (m, 2H), 3.70 (t, J = 5.8 Hz, 2H), c]pyridine-2-carboxamide 3.42 (td, J = 11.4, 2.5 Hz, 2H), 2.92 (m, 1H), 2.50 (m, 2H), 1.72-1.52 (m, 4H) 707 N-{4-[1-(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 435 tetrahydropyridin-4- 1H), 7.53 (m, 2H), 7.38 (d, J = 4.9 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.32 (m, 2H), 6.06 (m, 1H), 4.80 (m, 4H), 4.36 (dd, J = 9.2, 2H-pyrrolo[3,4- 2.9 Hz, 1H), 4.14 (s, 2H), 3.83-3.60 (m, c]pyridine-2-carboxamide 7H), 3.52 (m, 1H), 2.50 (m, 2H) 708 N-(4-{1-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpyrrolidin-3- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 432 yl)carbonyl]-1,2,3,6- 1H), 7.53 (m, 2H), 7.38 (dd, J = 5.0, 1.1 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.32 (m, 2H), 6.07 (m, 1H), 4.79 (m, 4H), yl}phenyl)-1,3-dihydro- 4.12 (m, 2H), 3.68 (t, J = 5.7 Hz, 2H), 3.27 (m, 1H), 2H-pyrrolo[3,4- 2.77 (t, J = 8.6 Hz, 1H), 2.62-2.45 (m, 2H), c]pyridine-2-carboxamide 2.50 (m, 2H), 2.38 (m, 1H), 2.24 (s, 3H), 1.97 (m, 2H) 709 N-(4-{1-[(1,1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dioxidotetrahydrothiophen- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 467 3-yl)carbonyl]-1,2,3,6- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.1 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.33 (m, 2H), 6.07 (m, 1H), 4.80 (m, 4H), 4.17 (bs, yl}phenyl)-1,3-dihydro- 2H), 3.72 (m, 3H), 3.31-3.13 (m, 3H), 3.07 (m, 2H-pyrrolo[3,4- 1H), 2.51 (bs, 2H), 2.35 (m, 1H), 2.13 (m, 1H) c]pyridine-2-carboxamide 710 N-{4-[1-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpropanoyl)- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), m/e 407 1,2,3,6-tetrahydropyridin- 8.20 (bs, 1H), 7.52 (m, 2H), 7.38 (d, J = 5.0 Hz, 1H), (M + H)⁺ 4-yl]phenyl}-1,3- 7.33 (m, 2H), 6.08 (bs, 1H), 5.09 (s, 1H), 4.82 (m, dihydro-2H-pyrrolo[3,4- 4H), 4.28 (m, 2H), 3.93 (m, 2H), 2.51 (m, 2H), c]pyridine-2-carboxamide 1.36 (s, 6H) 799 N-{4-[1-(morpholin-4- ¹H NMR (501 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylacetyl)-1,2,3,6- ppm 8.59 (s, 1H), 8.49 (d, J = 5.0 Hz, 1H), m/e tetrahydropyridin-4- 8.25 (bs, 1H), 7.54 (m, 2H), 7.39 (d, J = 5.1 Hz, 1H), XXX yl]phenyl}-1,3-dihydro- 7.35 (s, 1H), 7.33 (s, 1H), 6.08 (m, 1H), 4.82 (bs, (M + H)⁺ 2H-pyrrolo[3,4- 2H), 4.80 (bs, 2H), 4.18 (m, 2H), 3.71 (m, 2H), c]pyridine-2-carboxamide 3.58 (m, 4H), 3.21 (bs, 2H), 2.52 (m, 2H), 2.45 (m, 4H) 967 N-(4-{1-[(2R)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) tetrahydrofuran-2- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), m/e 419 ylcarbonyl]-1,2,3,6- 8.21 (bs, 1H), 7.53 (m, 2H), 7.38 (d, J = 5.1 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.33 (m, 2H), 6.07 (m, 1H), 4.80 (m, 4H), 4.67 (t, yl}phenyl)-1,3-dihydro- J = 6.5 Hz, 1H), 4.14 (m, 2H), 3.86-3.64 (m, 2H-pyrrolo[3,4- 4H), 2.50 (m, 2H), 2.11 (m, 1H), 2.00 (m, 1H), c]pyridine-2-carboxamide 1.86 (m, 2H) 968 N-(4-{1-[(2S)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) tetrahydrofuran-2- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 419 ylcarbonyl]-1,2,3,6- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.0 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.32 (m, 2H), 6.07 (m, 1H), 4.79 (m, 4H), 4.67 (dd, J = 7.5, yl}phenyl)-1,3-dihydro- 5.6 Hz, 1H), 4.14 (m, 2H), 3.85-3.66 (m, 2H-pyrrolo[3,4- 4H), 2.50 (m, 2H), 2.11 (m, 1H), 2.00 (m, 1H), c]pyridine-2-carboxamide 1.86 (m, 2H) 1014 N-(4-{1-[(1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpiperidin-4- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), m/e 446 yl)carbonyl]-1,2,3,6- 8.20 (bs, 1H), 7.53 (m, 2H), 7.38 (d, J = 5.0 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.32 (m, 2H), 6.07 (bs, 1H), 4.82 (m, 4H), yl}phenyl)-1,3-dihydro- 4.12 (m, 2H), 3.67 (t, J = 5.7 Hz, 2H), 2.76 (m, 2H), 2H-pyrrolo[3,4- 2.55 (m, 1H), 2.50 (m, 2H), 2.16 (s, 3H), 1.95 (td, c]pyridine-2-carboxamide J = 11.2, 3.6 Hz, 2H), 1.62 (m, 4H) 1015 N-(4-{1-[(1,1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dioxidotetrahydro-2H- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 481 thiopyran-4-yl)carbonyl]- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.0 Hz, 1H), (M + H)⁺ 1,2,3,6-tetrahydropyridin- 7.33 (m, 2H), 6.08 (m, 1H), 4.82 (m, 4H), 4.15 (m, 4-yl}phenyl)-1,3- 2H), 3.71 (t, J = 5.7 Hz, 2H), 3.24-3.04 (m, 5H), dihydro-2H-pyrrolo[3,4- 2.50 (m, 2H), 2.06 (m, 4H) c]pyridine-2-carboxamide 1016 N-(4-{1-[(3R)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) tetrahydrofuran-3- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 419 ylcarbonyl]-1,2,3,6- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.1 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.33 (m, 2H), 6.07 (m, 1H), 4.79 (m, 4H), 4.14 (m, yl}phenyl)-1,3-dihydro- 2H), 3.91 (t, J = 8.1 Hz, 1H), 3.77-3.67 (m, 5H), 2H-pyrrolo[3,4- 3.38 (m, 1H), 2.50 (m, 2H), 2.05 (m, 2H) c]pyridine-2-carboxamide 1017 N-(4-{1-[(3S)- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) tetrahydrofuran-3- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 419 ylcarbonyl]-1,2,3,6- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.1 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.33 (m, 2H), 6.07 (m, 1H), 4.79 (m, 4H), 4.14 (m, yl}phenyl)-1,3-dihydro- 2H), 3.91 (t, J = 8.1 Hz, 1H), 3.78-3.64 (m, 5H), 2H-pyrrolo[3,4- 3.38 (m, 1H), 2.50 (m, 2H), 2.05 (m, 2H) c]pyridine-2-carboxamide 1077 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 3-ylacetyl)-1,2,3,6- ppm 8.57 (bs, 1H), 8.48 (d, J = 5.0 Hz, 1H), m/e 433 tetrahydropyridin-4- 8.20 (s, 1H), 7.53 (m, 2H), 7.37 (m, 1H), 7.32 (m, 2H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 6.06 (m, 1H), 4.81 (m, 4H), 4.11 (d, J = 2.8 Hz, 2H-pyrrolo[3,4- 2H), 3.82 (dd, J = 8.4, 6.8 Hz, 1H), c]pyridine-2-carboxamide 3.76-3.59 (m, 4H), 3.29 (dd, J = 8.4, 6.1 Hz, 1H), 2.58-2.40 (m, 5H), 2.02 (m, 1H), 1.53 (m, 1H) 1078 N-{4-[1-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-4-ylacetyl)-1,2,3,6- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 447 tetrahydropyridin-4- 1H), 7.52 (m, 2H), 7.38 (d, J = 5.1 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.32 (m, 2H), 6.07 (m, 1H), 4.80 (m, 4H), 4.11 (m, 2H-pyrrolo[3,4- 2H), 3.81 (m, 2H), 3.67 (t, J = 5.7 Hz, 2H), c]pyridine-2-carboxamide 3.30 (td, J = 11.5, 2.2 Hz, 2H), 2.50 (m, 2H), 2.31 (d, J = 6.8 Hz, 2H), 2.98 (m, 1H), 1.62 (m, 2H), 1.25 (m, 2H) 1079 N-{4-[1-(N,N- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) dimethylglycyl)-1,2,3,6- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 406 tetrahydropyridin-4- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.1 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.33 (m, 2H), 6.07 (m, 1H), 4.80 (m, 4H), 4.15 (m, 2H-pyrrolo[3,4- 2H), 3.70 (t, J = 5.7 Hz, 2H), 3.15 (s, 2H), c]pyridine-2-carboxamide 2.50 (m, 2H), 2.23 (s, 6H) 1080 N-(4-{1-[(4- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylpiperazin-1- ppm 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.20 (s, m/e 461 yl)acetyl]-1,2,3,6- 1H), 7.53 (m, 2H), 7.38 (d, J = 5.1 Hz, 1H), (M + H)⁺ tetrahydropyridin-4- 7.32 (m, 2H), 6.06 (m, 1H), 4.80 (m, 4H), 4.15 (m, yl}phenyl)-1,3-dihydro- 2H), 3.71 (m, 2H), 3.19 (m, 4H), 2.44 (m, 4H), 2H-pyrrolo[3,4- 2.33 (m, 4H), 2.15 (s, 3H) c]pyridine-2-carboxamide 1254 N-{4-[1-(3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methylbutanoyl)-1,2,3,6- ppm 8.59 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 405 tetrahydropyridin-4- 1H), 7.53 (m, 2H), 7.39 (d, J = 5.1 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.33 (m, 2H), 6.07 (m, 1H), 4.81 (m, 4H), 4.12 (m, 2H-pyrrolo[3,4- 2H), 3.67 (t, J = 5.7 Hz, 2H), 2.50 (m, 2H), c]pyridine-2-carboxamide 2.25 (d, J = 6.9 Hz, 2H), 2.05 (m, 1H), 0.94 (d, J = 6.6 Hz, 6H) 1255 N-{4-[1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (cyclopentylacetyl)- ppm 8.59 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 431 1,2,3,6-tetrahydropyridin- 1H), 7.53 (m, 2H), 7.39 (d, J = 5.1 Hz, 1H), (M + H)⁺ 4-yl]phenyl}-1,3- 7.33 (m, 2H), 6.07 (m, 1H), 4.82 (m, 4H), 4.11 (m, dihydro-2H-pyrrolo[3,4- 2H), 3.67 (t, J = 5.7 Hz, 2H), 2.50 (m, 2H), c]pyridine-2-carboxamide 2.38 (d, J = 7.1 Hz, 2H), 2.21 (m, 1H), 1.77 (m, 2H), 1.66-1.46 (m, 4H), 1.18 (m, 2H) 1256 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 2-ylacetyl)-1,2,3,6- ppm 8.59 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 433 tetrahydropyridin-4- 1H), 7.53 (m, 2H), 7.39 (d, J = 5.0 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.33 (m, 2H), 6.07 (m, 1H), 4.80 (m, 4H), 4.16 (m, 2H-pyrrolo[3,4- 3H), 3.77 (m, 1H), 3.68 (m, 2H), 3.60 (m, 1H), c]pyridine-2-carboxamide 2.69 (m, 1H), 2.50 (m, 2H), 2.45 (m, 1H), 2.02 (m, 1H), 1.83 (m, 2H), 1.54 (m, 1H) 1257 N-{4-[1-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-2-ylacetyl)-1,2,3,6- ppm 8.59 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.21 (s, m/e 447 tetrahydropyridin-4- 1H), 7.53 (m, 2H), 7.39 (d, J = 5.0 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.33 (m, 2H), 6.06 (m, 1H), 4.83 (m, 4H), 4.12 (m, 2H-pyrrolo[3,4- 2H), 3.83 (m, 1H), 3.69 (m, 3H), 3.35 (m, 1H), c]pyridine-2-carboxamide 2.61 (m, 1H), 2.50 (m, 2H), 2.37 (m, 1H), 1.82-1.63 (m, 2H), 1.48 (m, 3H), 1.26 (m, 1H) 1258 N-{4-[1-(pyrrolidin-1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylacetyl)-1,2,3,6- ppm 8.59 (s, 1H), 8.48 (d, J = 5.0 Hz, 1H), m/e 432 tetrahydropyridin-4- 8.21 (bs, 1H), 7.53 (m, 2H), 7.39 (d, J = 5.0 Hz, 1H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.33 (m, 2H), 6.07 (bs, 1H), 4.81 (m, 4H), 2H-pyrrolo[3,4- 4.15 (m, 2H), 3.71 (m, 2H), 3.32 (bs, 2H), 2.55 (m, c]pyridine-2-carboxamide 4H), 2.50 (m, 2H), 1.70 (m, 4H) 1259 N-{4-[1-(pyrazin-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.85 (d, J = 1.5 Hz, 1H), 8.72 (d, J = 2.5 Hz, m/e 427 tetrahydropyridin-4- 1H), 8.66 (m, 1H), 8.58 (s, 1H), 8.48 (d, J = 5.0 Hz, (M + H)⁺ yl]phenyl}-1,3-dihydro- 1H), 8.22 (s, 1H), 7.53 (m, 2H), 7.38 (d, J = 5.1 Hz, 2H-pyrrolo[3,4- 1H), 7.34 (m, 2H), 6.09 (m, 1H), 4.82 (m, c]pyridine-2-carboxamide 4H), 4.22 (m, 2H), 3.69 (m, 2H), 2.57 (m, 2H) 1479 N-(4-{1-[(2-methyl-1,3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) oxazol-4-yl)carbonyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 8.25 (s, m/e 430 1,2,3,6-tetrahydropyridin- 1H) 7.49-7.54 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 4-yl}phenyl)-1,3- 7.33-7.37 (m, 2H) 6.11 (t, J = 3.51 Hz, 1H) dihydro-2H-pyrrolo[3,4- 4.82 (d, J = 7.93 Hz, 4H) 4.36 (s, 2H) 3.95 (s, 2H) c]pyridine-2-carboxamide 2.53-2.59 (m, 2H) 2.45-2.47 (m, 3H) 1480 N-{4-[1-(furan-3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.59 (s, 1H) 8.49 (d, J = 5.19 Hz, 1H) 7.98 (s, m/e 415 tetrahydropyridin-4- 1H) 7.67 (t, J = 1.68 Hz, 1H) 7.52 (d, J = 8.54 Hz, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H) 7.43 (d, J = 4.88 Hz, 1H) 7.35 (d, J = 8.54 Hz, 2H-pyrrolo[3,4- 2H) 6.69 (s, 1H) 6.05-6.13 (m, 1H) 4.82 (d, 4 c]pyridine-2-carboxamide H) 4.23-4.28 (m, 2H) 3.79 (t, J = 5.80 Hz, 2H) 2.53-2.59 (m, 2H) 1481 N-(4-{1-[(2E)-3-(furan-2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) yl)prop-2-enoyl]-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 441 tetrahydropyridin-4- 7.70 (d, J = 1.53 Hz, 1H) 7.49-7.55 (m, 2H) (M + H)⁺ yl}phenyl)-1,3-dihydro- 7.30-7.44 (m, 4H) 6.91 (d, J = 15.26 Hz, 1H) 6.81 (d, 2H-pyrrolo[3,4- J = 3.36 Hz, 1H) 6.57 (dd, J = 3.36, 1.83 Hz, 1H) c]pyridine-2-carboxamide 6.12 (t, J = 3.51 Hz, 1H) 4.81 (d, 4H) 4.24-4.28 (m, 2H) 3.81 (t, J = 5.65 Hz, 2H) 2.55 (s, 2H) 1482 N-{4-[1-(1,3-oxazol-5- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.59 (s, 1H) 8.49 (d, J = 4.88 Hz, 1H) 8.41 (s, m/e 416 tetrahydropyridin-4- 1H) 7.67 (s, 1H) 7.52 (d, J = 8.85 Hz, 2H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.44 (d, J = 5.19 Hz, 1H) 7.36 (d, J = 8.54 Hz, 2H) 2H-pyrrolo[3,4- 6.09-6.14 (m, 1H) 4.83 (d, J = 4.88 Hz, 4H) 4.32 (d, c]pyridine-2-carboxamide J = 2.75 Hz, 2H) 3.87 (t, J = 5.80 Hz, 2H) 2.60 (m, 2H) 1483 N-{4-[1-(3,3,3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) trifluoropropanoyl)- ppm 8.58 (s, 1H) 8.48 (d, 1H) 7.52 (d, J = 8.85 Hz, m/e 431 1,2,3,6-tetrahydropyridin- 2H) 7.42 (d, 1H) 7.35 (d, J = 8.85 Hz, 2H) (M + H)⁺ 4-yl]phenyl}-1,3- 6.08 (s, 1H) 4.81 (d, J = 9.16 Hz, 4H) dihydro-2H-pyrrolo[3,4- 4.12-4.16 (m, 2H) 3.65-3.73 (m, 2H) 3.51-3.63 (m, 2H) c]pyridine-2-carboxamide 2.52-2.58 (m, 2H) 1484 N-(4-{1-[(1,5-dimethyl- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) 1H-pyrazol-3- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 443 yl)carbonyl]-1,2,3,6- 7.51 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ tetrahydropyridin-4- 7.35 (d, J = 8.54 Hz, 2H) 6.33 (s, 1H) 6.07-6.12 (m, 1 yl}phenyl)-1,3-dihydro- H) 4.81 (d, J = 7.32 Hz, 4H) 4.36 (s, 2H) 3.94 (s, 2H-pyrrolo[3,4- 2H) 3.75-3.78 (m, 3H) 2.52-2.57 (m, 2H) c]pyridine-2-carboxamide 2.26-2.29 (m, 3H) 1485 N-(4-{1-[(4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methoxycyclohexyl)carbonyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 461 1,2,3,6- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ tetrahydropyridin-4- 7.34 (d, J = 8.54 Hz, 2H) 6.09 (t, J = 3.51 Hz, 1H) yl}phenyl)-1,3-dihydro- 4.81 (d, J = 7.63 Hz, 4H) 4.12 (s, 2H) 3.68 (t, J = 5.80 Hz, 2H-pyrrolo[3,4- 2H) 3.37-3.43 (m, 1H) 3.22 (s, 3H) c]pyridine-2-carboxamide 2.61-2.74 (m, 1H) 2.44-2.50 (m, 2H) 1.82-1.91 (m, J = 12.97, 3.81 Hz, 2H) 1.62-1.75 (m, 2H) 1.37-1.55 (m, 4H) 1486 N-{4-[1-(2,3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) dimethylbutanoyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 419 1,2,3,6-tetrahydropyridin- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.34 (d, J = 8.54 Hz, 2H) 6.07-6.13 (m, 1H) 4.81 (d, dihydro-2H-pyrrolo[3,4- J = 7.63 Hz, 4H) 4.15 (s, 2H) 3.66-3.76 (m, 2H) c]pyridine-2-carboxamide 2.56-2.65 (m, 1H) 2.42-2.50 (m, 2H) 1.74-1.89 (m, 1H) 1.00 (d, J = 6.71 Hz, 3H) 0.87 (dd, J = 13.58, 6.87 Hz, 6H) 1487 N-(4-{1-[(2,2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) difluorocyclopropyl)carbonyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 425 1,2,3,6- 7.52 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ tetrahydropyridin-4- 7.35 (d, J = 8.85 Hz, 2H) 6.10 (s, 1H) 4.82 (d, J = 7.32 Hz, yl}phenyl)-1,3-dihydro- 4H) 4.19 (s, 2H) 3.65-3.94 (m, 2H) 2H-pyrrolo[3,4- 2.94-3.16 (m, J = 7.32 Hz, 1H) 2.52-2.66 (m, 2H) c]pyridine-2-carboxamide 1.91-2.00 (m, 1H) 1.76-1.88 (m, 1H) 1488 N-{4-[1-(1H-pyrazol-5- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) ylcarbonyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 415 tetrahydropyridin-4- 7.71 (d, J = 2.14 Hz, 1H) 7.33-7.55 (m, 5H) 6.59 (d, (M + H)⁺ yl]phenyl}-1,3-dihydro- J = 2.44 Hz, 1H) 6.11 (s, 1H) 4.82 (d, J = 6.41 Hz, 2H-pyrrolo[3,4- 4H) 4.37 (s, 2H) 3.95 (s, 2H) 2.53-2.59 (m, c]pyridine-2-carboxamide J = 3.05 Hz, 2H) 1489 N-{4-[1-(tert- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) butoxyacetyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 435 tetrahydropyridin-4- 7.51 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.34 (d, J = 8.54 Hz, 2H) 6.08 (t, J = 3.36 Hz, 1H) 2H-pyrrolo[3,4- 4.82 (d, J = 7.93 Hz, 4H) 4.12 (s, 2H) 4.05 (s, 2H) c]pyridine-2-carboxamide 3.69 (t, J = 5.80 Hz, 2H) 1.19 (s, 9H) 1490 N-(4-{1-[3-(1H-1,2,4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) triazol-1-yl)propanoyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 8.39 (s, m/e 444 1,2,3,6-tetrahydropyridin- 1 H) 7.88 (s, 1H) 7.48-7.53 (m, 2H) 7.42 (d, (M + H)⁺ 4-yl}phenyl)-1,3- J = 4.88 Hz, 1H) 7.33 (d, J = 8.54 Hz, 2H) 6.05 (s, dihydro-2H-pyrrolo[3,4- 1H) 4.82 (d, J = 6.41 Hz, 4H) 4.46 (t, J = 6.71 Hz, c]pyridine-2-carboxamide 2H) 4.07-4.12 (m, 2H) 3.60-3.67 (m, 2H) 2.98 (t, J = 6.26 Hz, 2H) 2.42-2.49 (m, 2H) 1491 N-{4-[1-(3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) ethoxypropanoyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 421 1,2,3,6-tetrahydropyridin- 7.51 (d, J = 8.54 Hz, 2H) 7.42 (d, J = 5.19 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.34 (d, J = 8.54 Hz, 2H) 6.06-6.10 (m, 1H) 4.82 (d, dihydro-2H-pyrrolo[3,4- J = 7.63 Hz, 4H) 4.13 (s, 2H) 3.62-3.72 (m, 4H) c]pyridine-2-carboxamide 3.44 (q, J = 7.22 Hz, 2H) 2.57-2.65 (m, 2H) 1.09 (t, J = 6.87 Hz, 3H) 1492 N-{4-[1-(3-hydroxy-3- ¹H NMR (400 MHz, Solvent) δ ppm 8.58 (s, 1H) (ESI(+)) methylbutanoyl)-1,2,3,6- 8.48 (d, J = 5.19 Hz, 1H) 7.49-7.54 (m, 2H) m/e 421 tetrahydropyridin-4- 7.41 (d, J = 4.88 Hz, 1H) 7.34 (d, J = 8.54 Hz, 2H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 6.08 (s, 1H) 4.81 (d, J = 7.63 Hz, 4H) 4.16 (s, 2H) 2H-pyrrolo[3,4- 3.72 (t, J = 5.80 Hz, 2H) 2.31-2.50 (m, J = 14.04 Hz, c]pyridine-2-carboxamide 2H) 1.12-1.33 (m, 8H) 1493 N-(4-{1-[3-(1H-pyrrol-1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) yl)propanoyl]-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 442 tetrahydropyridin-4- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ yl}phenyl)-1,3-dihydro- 7.32 (d, J = 8.54 Hz, 2H) 6.72 (t, J = 1.98 Hz, 2H) 2H-pyrrolo[3,4- 6.04 (t, 1H) 5.96 (t, J = 2.14 Hz, 2H) 4.81 (d, J = 7.93 Hz, c]pyridine-2-carboxamide 4H) 4.16 (t, J = 6.87 Hz, 2H) 4.06 (t, 2H) 3.63 (s, 2H) 2.82 (s, 2H) 2.45 (s, 2H) 1494 N-(4-{1-[(1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methylcyclopropyl)carbonyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 403 1,2,3,6- 7.48-7.54 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ tetrahydropyridin-4- 7.32-7.37 (m, 2H) 6.11 (t, J = 3.51 Hz, 1H) 4.79-4.85 (m, 4 yl}phenyl)-1,3-dihydro- H) 4.12-4.20 (m, 2H) 3.78 (t, J = 5.65 Hz, 2H) 2H-pyrrolo[3,4- 2.47-2.51 (m, 2H) 1.26-1.30 (m, 3H) c]pyridine-2-carboxamide 0.81-0.86 (m, 2H) 0.55-0.62 (m, 2H) 1495 N-(4-{1-[(2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methylpropoxy)acetyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 435 1,2,3,6-tetrahydropyridin- 7.48-7.53 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 4-yl}phenyl)-1,3- 7.31-7.35 (m, 2H) 6.05-6.09 (m, 1H) 4.82 (d, J = 7.93 Hz, dihydro-2H-pyrrolo[3,4- 4H) 4.07-4.20 (m, 4H) 3.67 (t, J = 5.65 Hz, 2H) c]pyridine-2-carboxamide 3.18-3.24 (m, 2H) 2.47-2.51 (m, 2H) 1.76-1.89 (m, 1H) 0.85-0.91 (m, 6H) 1496 N-{4-[1-(1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methylprolyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 432 tetrahydropyridin-4- 7.49-7.54 (m, 2H) 7.41 (d, J = 5.19 Hz, 1H) 7.34 (d, (M + H)⁺ yl]phenyl}-1,3-dihydro- J = 8.85 Hz, 2H) 6.09 (t, J = 3.36 Hz, 1H) 2H-pyrrolo[3,4- 4.78-4.84 (m, 4H) 4.19 (s, 2 H) 3.66-3.89 (m, 2H) c]pyridine-2-carboxamide 3.30-3.35 (m, 1H) 2.98-3.06 (m, 1H) 2.43-2.50 (m, 2H) 2.29-2.37 (m, 1H) 2.27 (s, 3H) 2.05-2.14 (m, 1H) 1.71-1.86 (m, 3H) 1497 N-{4-[1-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methylbutanoyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 421 tetrahydropyridin-4- 7.49-7.53 (m, 2H) 7.41 (d, J = 5.19 Hz, 1H) 7.34 (d, (M + H)⁺ yl]phenyl}-1,3-dihydro- J = 8.85 Hz, 2H) 6.09 (t, J = 3.66 Hz, 1H) 4.81 (d, 2H-pyrrolo[3,4- J = 7.02 Hz, 4H) 4.29 (s, 2H) 3.85-3.98 (m, 2H) c]pyridine-2-carboxamide 2.46-2.51 (m, 2H) 1.59-1.86 (m, 2H) 1.32-1.35 (m, 3H) 0.82 (t, 3H) 1498 N-(4-{1-[(1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) hydroxycyclopropyl)carbonyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 405 1,2,3,6- 7.51 (d, J = 8.54 Hz, 2H) 7.42 (d, J = 5.19 Hz, 1H) (M + H)⁺ tetrahydropyridin-4- 7.33-7.37 (m, 2H) 6.11 (t, J = 3.36 Hz, 1H) 4.82 (d, yl}phenyl)-1,3-dihydro- J = 6.41 Hz, 4H) 4.24 (s, 2H) 3.87 (t, J = 5.65 Hz, 2 2H-pyrrolo[3,4- H) 2.52-2.57 (m, 2H) 0.93-0.99 (m, 2H) c]pyridine-2-carboxamide 0.80-0.85 (m, 2H) 1499 N-{4-[1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) (cyclopropylacetyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 403 1,2,3,6-tetrahydropyridin- 7.51 (d, J = 8.85 Hz, 2H) 7.42 (d, J = 5.19 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.31-7.37 (m, 2H) 6.05-6.11 (m, 1H) 4.82 (d, dihydro-2H-pyrrolo[3,4- J = 6.41 Hz, 4H) 4.09-4.13 (m, J = 3.05 Hz, 2H) c]pyridine-2-carboxamide 3.67 (t, J = 5.80 Hz, 2H) 2.46-2.50 (m, 2H) 2.33 (d, J = 6.71 Hz, 2H) 1.00 (s, 1H) 0.44-0.51 (m, 2 H) 0.16 (q, J = 4.98 Hz, 2H) 1500 N-{4-[1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) (cyclopentylcarbonyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 417 1,2,3,6-tetrahydropyridin- 7.49-7.53 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.31-7.36 (m, 2H) 6.04-6.12 (m, 1H) 4.79-4.84 (m, 4H) dihydro-2H-pyrrolo[3,4- 4.14 (s, 2H) 3.70 (t, J = 5.80 Hz, 2H) 3.02 (m, c]pyridine-2-carboxamide J = 7.63 Hz, 1H) 2.43-2.49 (m, 2H) 1.48-1.86 (m, 8H) 1501 N-[4-(1-{[1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) (methoxymethyl)cyclopropyl]carbonyl}- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 433 1,2,3,6- 7.48-7.55 (m, 2H) 7.41 (d, J = 5.19 Hz, 1H) 7.34 (d, (M + H)⁺ tetrahydropyridin-4- J = 8.85 Hz, 2H) 6.06-6.12 (m, J = 3.51, 3.51 Hz, 1 yl)phenyl]-1,3-dihydro- H) 4.79-4.85 (m, 4H) 4.17 (d, J = 3.05 Hz, 2H) 2H-pyrrolo[3,4- 3.79 (t, J = 5.80 Hz, 2H) 3.44 (s, 2H) 3.25 (s, 3H) c]pyridine-2-carboxamide 2.46-2.50 (m, 2H) 0.85-0.90 (m, 2H) 0.73-0.80 (m, 2H) 1502 N-(4-{1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) [(methylsulfonyl)acetyl]- ppm 8.59 (s, 1H) 8.49 (d, J = 5.19 Hz, 1H) m/e 441 1,2,3,6-tetrahydropyridin- 7.52 (d, J = 8.85 Hz, 2H) 7.42 (d, J = 5.49 Hz, 1H) (M + H)⁺ 4-yl}phenyl)-1,3- 7.32-7.38 (m, J = 8.85 Hz, 2H) 6.08 (s, 1H) 4.82 (d, dihydro-2H-pyrrolo[3,4- J = 6.10 Hz, 4H) 4.35-4.46 (m, 2H) c]pyridine-2-carboxamide 4.11-4.26 (m, 2H) 3.74 (t, J = 5.80 Hz, 2H) 3.08-3.12 (m, 3 H) 2.53-2.69 (m, 2H) 1503 N-(4-{1-[(1-methyl-1H- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) pyrazol-4-yl)carbonyl]- ppm 8.59 (s, 1H) 8.49 (d, J = 4.88 Hz, 1H) 8.00 (s, m/e 429 1,2,3,6-tetrahydropyridin- 1H) 7.69 (s, 1H) 7.49-7.54 (m, 2H) 7.42 (d, (M + H)⁺ 4-yl}phenyl)-1,3- J = 5.49 Hz, 1H) 7.33-7.38 (m, 2H) dihydro-2H-pyrrolo[3,4- 6.07-6.12 (m, J = 3.51, 3.51 Hz, 1H) 4.79-4.85 (m, 4H) c]pyridine-2-carboxamide 4.27 (d, J = 3.05 Hz, 2H) 3.87 (s, 3H) 3.81 (t, J = 5.65 Hz, 2H) 2.54-2.61 (m, J = 3.36 Hz, 2H) 1504 N-[4-(1-acetyl-1,2,3,6- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) tetrahydropyridin-4- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 363 yl)phenyl]-1,3-dihydro- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 2H-pyrrolo[3,4- 7.34 (d, J = 8.54 Hz, 2H) 6.08 (t, J = 3.51 Hz, 1H) c]pyridine-2-carboxamide 4.82 (d, J = 7.32 Hz, 4H) 4.10 (s, 2H) 3.65 (t, J = 5.80 Hz, 2H) 2.41-2.51 (m, 2H) 2.06 (s, 3H) 1505 N-{4-[1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) (cyclopropylcarbonyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 389 1,2,3,6-tetrahydropyridin- 7.52 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 4.58 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.35 (d, J = 8.85 Hz, 2H) 6.10 (s, 1H) 4.81 (d, J = 8.54 Hz, dihydro-2H-pyrrolo[3,4- 4H) 4.22 (s, 2H) 3.71-3.84 (m, 2H) c]pyridine-2-carboxamide 2.37-2.49 (m, 2H) 1.90-2.01 (m, J = 13.73 Hz, 1H) 0.71-0.84 (m, 4H) 1506 N-{4-[1-(2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) ethylbutanoyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 419 tetrahydropyridin-4- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.34 (d, J = 8.85 Hz, 2H) 6.08-6.12 (m, 1H) 4.81 (d, 2H-pyrrolo[3,4- J = 7.93 Hz, 4H) 4.14-4.20 (m, J = 1.83 Hz, 2H) c]pyridine-2-carboxamide 3.74 (t, J = 5.80 Hz, 2H) 2.60-2.71 (m, 1H) 2.43-2.50 (m, 2H) 1.37-1.62 (m, 4H) 0.82 (t, J = 7.32 Hz, 6H) 1507 N-{4-[1-(5-oxo-L- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) prolyl)-1,2,3,6- ppm 8.59 (s, 1H) 8.49 (d, J = 4.88 Hz, 1H) m/e 432 tetrahydropyridin-4- 7.52 (d, J = 8.85 Hz, 2H) 7.43 (d, J = 4.88 Hz, 1H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.35 (d, J = 8.85 Hz, 2H) 6.09 (s, 1H) 4.82 (d, J = 6.71 Hz, 2H-pyrrolo[3,4- 4H) 4.58 (s, 1H) 4.14 (s, 2H) 3.70 (t, 2H) c]pyridine-2-carboxamide 2.55-2.64 (m, 1H) 2.29-2.46 (m, 2H) 2.14-2.22 (m, 2H) 1.92 (s, 1H) 1508 N-(4-{1-[(2E)-4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methylpent-2-enoyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 417 1,2,3,6-tetrahydropyridin- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ 4-yl}phenyl)-1,3- 7.34 (d, J = 8.85 Hz, 2H) 6.66 (dd, J = 15.26, 6.71 Hz, 1 dihydro-2H-pyrrolo[3,4- H) 6.34 (d, J = 15.26 Hz, 1H) 6.06-6.11 (m, 1H) c]pyridine-2-carboxamide 4.81 (d, J = 7.32 Hz, 4H) 4.18 (d, J = 2.75 Hz, 2H) 3.74 (t, J = 5.80 Hz, 2H) 2.38-2.50 (m, 3H) 1.05 (d, J = 6.71 Hz, 6H) 1509 N-{4-[1-(2-methoxy-2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methylpropanoyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 421 1,2,3,6-tetrahydropyridin- 7.51 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 4.58 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.35 (d, J = 8.85 Hz, 2H) 6.07-6.14 (m, 1H) dihydro-2H-pyrrolo[3,4- 4.78-4.84 (m, 4H) 4.31 (s, 2H) 3.92 (s, 2H) 3.16 (s, 3 c]pyridine-2-carboxamide H) 2.47-2.50 (m, 2H) 1.35-1.39 (m, 6H) 1510 N-{4-[1-(cyclopent-1-en- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) 1-ylcarbonyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 415 tetrahydropyridin-4- 7.51 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.32-7.37 (m, 2H) 6.06-6.11 (m, 1H) 2H-pyrrolo[3,4- 5.92-5.95 (m, 1H) 4.81 (d, J = 7.63 Hz, 4H) 4.15 (q, J = 2.64 Hz, c]pyridine-2-carboxamide 2H) 3.71 (t, J = 5.80 Hz, 2H) 2.53-2.57 (m, 2 H) 2.41-2.50 (m, 4H) 1.85-1.95 (m, 2H) 1511 N-{4-[1-(thiophen-3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (ESI(+)) ylacetyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 445 tetrahydropyridin-4- 7.50 (d, J = 8.54 Hz, 2H) 7.39-7.43 (m, J = 4.12, 4.12 Hz, (M + H)⁺ yl]phenyl}-1,3-dihydro- 2H) 7.31 (d, J = 8.85 Hz, 2H) 7.23 (s, 1H) 2H-pyrrolo[3,4- 7.02 (d, J = 5.19 Hz, 1H) 6.06 (s, 1H) 4.81 (d, c]pyridine-2-carboxamide J = 7.32 Hz, 4H) 4.15 (s, 2H) 3.77 (s, 2H) 3.70 (t, J = 5.80 Hz, 2H) 2.38-2.48 (m, 2H) 1512 N-{4-[1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) (cyclohexylcarbonyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 431 1,2,3,6-tetrahydropyridin- 7.49-7.53 (m, 2H) 7.41 (d, 1H) 7.34 (d, J = 8.54 Hz, 2 (M + H)⁺ 4-yl]phenyl}-1,3- H) 6.09 (s, 1H) 4.81 (d, 4H) 4.12 (s, 2H) 3.68 (t, dihydro-2H-pyrrolo[3,4- J = 5.95 Hz, 2H) 2.38-2.50 (m, 2H) c]pyridine-2-carboxamide 1.61-1.78 (m, 5H) 1.20-1.45 (m, 6H) 1513 N-[4-(1-propanoyl- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) 1,2,3,6-tetrahydropyridin- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 377 4-yl)phenyl]-1,3-dihydro- 7.51 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 2H-pyrrolo[3,4- 7.32-7.37 (m, 2H) 6.05-6.11 (m, 1H) 4.81 (d, c]pyridine-2-carboxamide J = 7.02 Hz, 4H) 4.11 (d, J = 3.05 Hz, 2H) 3.66 (t, J = 5.80 Hz, 2H) 2.45-2.50 (m, 2H) 2.33-2.41 (m, 2H) 1.05 (t, J = 7.32 Hz, 3H) 1514 N-{4-[1-(2,2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (ESI(+)) dimethylbutanoyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 419 1,2,3,6-tetrahydropyridin- 7.48-7.54 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.31-7.37 (m, 2H) 6.07-6.13 (m, 1H) 4.81 (d, J = 7.02 Hz, dihydro-2H-pyrrolo[3,4- 4H) 4.14-4.18 (m, 2H) 3.75 (t, J = 5.65 Hz, 2H) c]pyridine-2-carboxamide 2.45-2.50 (m, J = 1.83 Hz, 2H) 1.64 (q, J = 7.43 Hz, 2H) 1.18-1.23 (m, 6H) 0.81 (t, J = 7.48 Hz, 3 H) 1515 N-(4-{1-[(1-methyl-1H- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) pyrrol-2-yl)carbonyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 428 1,2,3,6-tetrahydropyridin- 7.52 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 4-yl}phenyl)-1,3- 7.36 (d, J = 8.85 Hz, 2H) 6.83-6.86 (m, 1H) 6.37 (dd, dihydro-2H-pyrrolo[3,4- J = 3.66, 1.53 Hz, 1H) 6.04-6.12 (m, 2H) 4.82 (d, c]pyridine-2-carboxamide J = 7.32 Hz, 4H) 4.24-4.28 (m, 2H) 3.82 (t, J = 5.80 Hz, 2H) 3.67 (s, 3H) 2.53-2.59 (m, J = 1.83 Hz, 2H) 1516 N-{4-[1-(methoxyacetyl)- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) 1,2,3,6-tetrahydropyridin- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 393 4-yl]phenyl}-1,3- 7.51 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ dihydro-2H-pyrrolo[3,4- 7.30-7.37 (m, 2H) 6.03-6.12 (m, 1H) 4.81 (d, c]pyridine-2-carboxamide J = 7.63 Hz, 4H) 4.00-4.17 (m, 4H) 3.57-3.70 (m, J = 5.65, 5.65 Hz, 2H) 3.31-3.37 (m, 3H) 2.41-2.50 (m, 2H) 1517 N-{4-[1-(2,2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) dimethylpropanoyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 405 1,2,3,6-tetrahydropyridin- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.34 (d, J = 8.85 Hz, 2H) 6.10 (t, J = 3.51 Hz, 1H) dihydro-2H-pyrrolo[3,4- 4.81 (d, J = 7.32 Hz, 4H) 4.16 (d, J = 3.05 Hz, 2H) c]pyridine-2-carboxamide 3.76 (t, J = 5.80 Hz, 2H) 2.46-2.50 (m, J = 1.83 Hz, 2 H) 1.25 (s, 9H) 1518 N-{4-[1-(4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) methylhexanoyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 433 tetrahydropyridin-4- 7.51 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.34 (d, J = 8.54 Hz, 2H) 6.05-6.11 (m, 1H) 4.82 (d, 2H-pyrrolo[3,4- J = 7.93 Hz, 4H) 4.08-4.16 (m, J = 1.53 Hz, 2H) c]pyridine-2-carboxamide 3.67 (t, J = 5.80 Hz, 2H) 2.43-2.50 (m, 2H) 2.30-2.40 (m, 2H) 1.50-1.68 (m, 1H) 1.27-1.45 (m, 3H) 1.10-1.22 (m, 1H) 0.80-0.91 (m, 6H) 1519 N-(4-{1-[(2,2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) dimethylcyclopropyl)carbonyl]- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 417 1,2,3,6- 7.47-7.53 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ tetrahydropyridin-4- 7.32-7.37 (m, 2H) 6.08-6.14 (m, 1H) 4.81 (d, 4H) 4.18 (s, yl}phenyl)-1,3-dihydro- 2H) 3.85-3.94 (m, 1H) 3.60 (s, 1H) 2H-pyrrolo[3,4- 2.39-2.50 (m, 2H) 1.73 (t, J = 7.32 Hz, 1H) 1.18-1.23 (m, 3 c]pyridine-2-carboxamide H) 0.96-1.01 (m, 1H) 0.96 (s, 3H) 0.68 (dd, J = 7.93, 3.97 Hz, 1H) 1520 N-(4-{1-[(1,3-dimethyl- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) 1H-pyrazol-5- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 443 yl)carbonyl]-1,2,3,6- 7.49-7.56 (m, 2H) 7.41 (d, J = 5.19 Hz, 1H) (M + H)⁺ tetrahydropyridin-4- 7.33-7.38 (m, 2H) 6.25 (s, 1H) 6.07-6.12 (m, 1H) 4.81 (d, yl}phenyl)-1,3-dihydro- J = 7.02 Hz, 4H) 4.18-4.24 (m, J = 2.75 Hz, 2H) 2H-pyrrolo[3,4- 3.72-3.79 (m, 5H) 2.53-2.60 (m, 2H) 2.18 (s, 3 c]pyridine-2-carboxamide H) 1521 N-{4-[1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) (cyclobutylacetyl)- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) m/e 417 1,2,3,6-tetrahydropyridin- 7.51 (d, J = 8.85 Hz, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ 4-yl]phenyl}-1,3- 7.34 (d, J = 8.85 Hz, 2H) 6.08 (t, J = 3.51 Hz, 1H) dihydro-2H-pyrrolo[3,4- 4.81 (d, J = 7.63 Hz, 4H) 4.10 (s, 2H) 3.62-3.69 (m, 2 c]pyridine-2-carboxamide H) 2.55-2.72 (m, 2H) 2.45-2.50 (m, 2H) 2.30-2.42 (m, 1H) 2.01-2.13 (m, 2H) 1.77-1.88 (m, 2H) 1.61-1.74 (m, 2H) 1522 N-{4-[1-(piperidin-1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) ylacetyl)-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 446 tetrahydropyridin-4- 7.48-7.55 (m, 2H) 7.41 (d, J = 4.58 Hz, 1H) (M + H)⁺ yl]phenyl}-1,3-dihydro- 7.31-7.36 (m, 2H) 6.08 (t, J = 3.36 Hz, 1H) 4.81 (d, 4H) 2H-pyrrolo[3,4- 4.14 (s, 2H) 3.66-3.78 (m, 2H) 3.16 (s, 2H) c]pyridine-2-carboxamide 2.46-2.51 (m, 2H) 2.36-2.43 (m, 4H) 1.45-1.59 (m, 4H) 1.32-1.43 (m, 2H) 1523 N-(4-{1-[2-(pyrrolidin-1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) yl)propanoyl]-1,2,3,6- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) m/e 446 tetrahydropyridin-4- 7.48-7.53 (m, 2H) 7.41 (d, J = 4.88 Hz, 1H) (M + H)⁺ yl}phenyl)-1,3-dihydro- 7.31-7.36 (m, 2H) 6.09 (t, J = 3.51 Hz, 1H) 4.81 (d, J = 7.02 Hz, 2H-pyrrolo[3,4- 4 H) 4.21 (s, 2H) 3.69-3.88 (m, 2H) c]pyridine-2-carboxamide 3.61-3.70 (m, 1H) 2.53-2.66 (m, 4H) 2.43-2.50 (m, 2H) 1.63-1.73 (m, 4H) 1.19 (d, J = 6.71 Hz, 3H) 1524 N-(4-{1-[(1,3-dimethyl- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.)δ (ESI(+)) 1H-pyrazol-4- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.78 (s, m/e 443 yl)carbonyl]-1,2,3,6- 1H) 7.52 (d, J = 8.54 Hz, 2H) 7.41 (d, J = 4.88 Hz, (M + H)⁺ tetrahydropyridin-4- 1H) 7.35 (d, J = 8.85 Hz, 2H) 6.07-6.11 (m, 1H) yl}phenyl)-1,3-dihydro- 4.81 (d, J = 7.32 Hz, 4H) 4.19 (d, J = 3.05 Hz, 2H) 2H-pyrrolo[3,4- 3.77-3.79 (m, 3H) 3.72-3.77 (m, 2H) c]pyridine-2-carboxamide 2.52-2.57 (m, 2H) 2.16-2.22 (m, 3H)

Example 547 N-[4-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-phenyl)-2,3-dihydro-isoindol-1-one. ESI-MS [M+H+]=370.1.

Example 548 N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 377C, substituting isoindoline with 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine. ESI-MS [M+H+]=384.1.

Example 549 N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide

The title compound was prepared as described in Example 377C, substituting isoindoline with 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine. ESI-MS [M+H+]=384.1.

Example 550 N-[4-(1-oxo-1,2-dihydroisoquinolin-4-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-cyclohex-1-enyl)-2H-isoquinolin-1-one. ESI-MS [M+H+]=386.2.

Example 551 N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-cyclohex-1-enyl)-2H-phthalazin-1-one. ESI-MS [M+H+]=387.2.

Example 552 N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)cyclohex-3-en-1-yl]-5-(pyrrolidin-1-ylmethyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 377C, substituting 4-(4-aminophenyl)-5,6,7,8-tetrahydro-2H-phthalazin-1-one with 4-(4-amino-cyclohex-1-enyl)-2H-phthalazin-1-one and isoindoline with 5-pyrrolidin-1-ylmethyl-2,3-dihydro-1H-isoindole. ESI-MS [M+H+]=470.2.

Example 557 N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 1-isopentyl-1H-pyrazol-4-amine dihydrochloride for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride in Example 272B. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.39 (s, 1H), 7.74 (s, 1H), 7.39 (s, 1H), 7.38-7.26 (m, 4H), 4.69 (s, 4H), 4.04 (t, J=7.1 Hz, 2H), 1.81-1.57 (m, 2H), 1.52-1.37 (m, 1H), 0.89 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 299 (M+H)⁺.

Example 558 N-[1-(2-phenylethyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 1-phenethyl-1H-pyrazol-4-amine dihydrochloride for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride in Example 272B. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.39 (s, 1H), 7.68 (s, 1H), 7.42 (s, 1H), 7.39-7.23 (m, 6H), 7.24-7.15 (m, 3H), 4.68 (bs, 4H), 4.27 (t, J=7.3 Hz, 2H), 3.07 (t, J=7.3 Hz, 2H); MS (ESI(+)) m/e 333 (M+H)⁺.

Example 559 N⁵-[2-(dimethylamino)ethyl]-N²-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2,5-dicarboxamide

The title compound was prepared as described in Example 1C, substituting N1,N1-dimethylethane-1,2-diamine for 3-phenylpropan-1-amine and 2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.28 (s, 1H), 8.70 (t, J=5.6 Hz, 1H), 8.62 (s, 1H), 8.26 (t, J=5.6 Hz, 1H), 7.86-7.74 (m, 4H), 7.68-7.61 (m, 2H), 7.49 (d, J=7.8 Hz, 1H), 4.84 (bs, 4H), 3.66-3.55 (m, 2H), 3.29-3.12 (m, 4H), 2.90-2.80 (m, 6H), 2.28-1.46 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 438 (M+H)⁺.

Example 560 5-(morpholin-4-ylcarbonyl)-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting morpholine for 3-phenylpropan-1-amine and 2-{[4-(propylcarbamoyl)phenyl]carbamoyl}isoindoline-5-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), 8.26 (t, J=5.7 Hz, 1H), 7.80-7.73 (m, 2H), 7.69-7.62 (m, 2H), 7.47-7.41 (m, 2H), 7.35 (dd, J=7.7, 1.6 Hz, 1H), 4.82 (bs, 4H), 3.73-3.43 (m, 6H), 3.28-3.12 (m, 4H), 1.60-1.44 (m, 2H), 0.89 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 437 (M+H)⁺.

Example 561 N-(4-{benzyl[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-benzyl-3-morpholinopropan-1-amine for 3-phenylpropan-1-amine. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.28 (s, 1H), 7.65-7.59 (m, 2H), 7.39-7.25 (m, 11H), 4.79 (bs, 4H), 4.63 (s, 2H), 3.52-3.45 (m, 4H), 3.35-3.27 (m, 2H), 2.27-2.20 (m, 4H), 2.17 (t, 2H), 1.69-1.60 (m, 2H); MS (ESI(+)) m/e 499 (M+H)⁺.

Example 563 5-bromo-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 563A 2-cyclopentyl-N-(4-nitrophenyl)acetamide

The title compound was prepared as described in Example 278, substituting 2-cyclopentylacetyl chloride for acetyl chloride and 4-nitroaniline for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide.

Example 563B N-(4-aminophenyl)-2-cyclopentylacetamide

The title compound was prepared as described in Example 274, substituting 2-cyclopentyl-N-(4-nitrophenyl)acetamide for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 563C 5-bromo-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting N-(4-aminophenyl)-2-cyclopentylacetamide for 4-amino-N-propylbenzamide and 5-bromoisoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.68 (s, 1H), 8.29 (s, 1H), 7.65-7.55 (m, 1H), 7.53-7.36 (m, 5H), 7.36-7.26 (m, 1H), 4.79-4.65 (m, 4H), 2.33-2.16 (m, 3H), 1.85-1.68 (m, 2H), 1.68-1.41 (m, 4H), 1.29-1.09 (m, 2H); MS (ESI(+)) m/e 442 (M+H)⁺.

Example 565 methyl 4-{[(5-cyano-1,3-dihydro-2H-isoindol-2-yl)carbonyl]amino}benzoate

The title compound was prepared as described in Example 1A, substituting 5-cyanoisoindoline for isoindoline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.81 (s, 1H), 7.91-7.82 (m, 3H), 7.82-7.77 (m, 1H), 7.76-7.69 (m, 2H), 7.59 (d, J=7.9 Hz, 1H), 4.89-4.81 (m, 4H), 3.81 (s, 3H); MS (ESI(+)) m/e 322 (M+H)⁺.

Example 566 N-(4-{(E)-[(benzyloxy)imino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 566A N-(4-formylphenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-aminobenzaldehyde for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.

Example 566B N-(4-{(E)-[(benzyloxy)imino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

In a 8 mL sealed vial was mixed N-(4-formylphenyl)isoindoline-2-carboxamide (50 mg, 0.188 mmol) in methanol (1 ml). A solution of O-benzylhydroxylamine hydrochloride (45.0 mg, 0.282 mmol) and sodium acetate (46.0 mg, 0.338 mmol) in water (1.000 ml) was then added and the reaction was stirred overnight at room temperature. The reaction was diluted with water and the product was extracted with dichloromethane. The organic layer was washed with brine, dried with sodium sulfate, decanted, and concentrated. Purification by chromatography provided the title compound. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.55 (s, 1H), 8.21 (s, 1H), 7.65 (m, 2H), 7.50 (m, 2H), 7.44-7.28 (m, 9H), 5.14 (s, 2H), 4.78 (bs, 4H); MS (ESI(+)) m/e 372 (M+H)⁺.

Example 573 N-[4-(3-aminopyrrolidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 339D. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 7.76 (bs, 1H), 7.36-7.31 (m, 2H), 7.31-7.25 (m, 4H), 6.46-6.42 (m, 2H), 4.73 (bs, 4H), 3.56 (p, J=5.8 Hz, 1H), 3.41-3.36 (m, 1H), 3.35-3.28 (m, 1H), 3.24-3.15 (m, 3H), 2.85 (dd, J=9.1, 4.9 Hz, 1H), 2.13-2.05 (m, 1H), 1.73-1.64 (m, 1H); MS (ESI(+)) m/e 323 (M+H)⁺.

Example 574 N-{6-[(3-methylbutyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 574A methyl 5-(isoindoline-2-carboxamido)picolinate

The title compound was prepared as described in Example 272B, substituting methyl 5-aminopicolinate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.

Example 574B 5-(isoindoline-2-carboxamido)picolinic acid

The title compound was prepared as described in Example 1B, substituting methyl 5-(isoindoline-2-carboxamido)picolinate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 574C N-{6-[(3-methylbutyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 5-(isoindoline-2-carboxamido)picolinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.85 (m, 2H), 8.57 (t, J=6.1 Hz, 1H), 8.17 (dd, J=8.5, 2.4 Hz, 1H), 7.94 (d, J=8.5 Hz, 1H), 7.41-7.29 (m, 4H), 4.79 (m, 4H), 3.35 (m, 2H), 1.59 (m, 1H), 1.42 (q, J=7.1 Hz, 2H), 0.90 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 353 (M+H)⁺.

Example 575 N-{6-[(3-phenylpropyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 5-(isoindoline-2-carboxamido)picolinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.86 (m, 2H), 8.68 (t, J=6.0 Hz, 1H), 8.18 (dd, J=8.6, 2.5 Hz, 1H), 7.95 (d, J=8.5 Hz, 1H), 7.41-7.14 (m, 9H), 4.81 (bs, 4H), 3.35 (m, 2H), 2.61 (t, J=7.6 Hz, 2H), 1.84 (m, 2H); MS (ESI(+)) m/e 401 (M+H)⁺.

Example 576 N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (tetrahydrofuran-3-yl)methanamine for 3-phenylpropan-1-amine and 5-(isoindoline-2-carboxamido)picolinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.87 (m, 2H), 8.78 (t, J=6.1 Hz, 1H), 8.18 (dd, J=8.5, 2.5 Hz, 1H), 7.95 (d, J=8.5 Hz, 1H), 7.42-7.26 (m, 4H), 4.81 (m, 4H), 3.75 (m, 1H), 3.70-3.56 (m, 2H), 3.47 (dd, J=8.5, 5.3 Hz, 1H), 3.27 (m, 2H), 2.53 (m, 1H), 1.91 (m, 1H), 1.61 (m, 1H); MS (ESI(+)) m/e 368 (M+H)⁺.

Example 577 N²-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2,5-dicarboxamide

The title compound was prepared as described in Example 132 substituting 5-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide for 5-cyano-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.69 (s, 1H), 8.31 (s, 1H), 7.98 (s, 1H), 7.87-7.78 (m, 2H), 7.53-7.38 (m, 5H), 7.36 (brs, 1H), 4.78 (bs, 4H), 2.32-2.13 (m, 3H), 1.82-1.67 (m, 2H), 1.67-1.42 (m, 4H), 1.27-1.10 (m, 2H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 578 N-[4-({benzyl[3-(morpholin-4-yl)propyl]amino}methyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

To a stirring suspension of N-(4-{benzyl[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide (0.028 g, 0.056 mmol) in THF (1.1 ml) was added 1M borane tetrahydrofuran complex (0.225 ml, 0.225 mmol) dropwise. The mixture was heated at 60° C. for 5 hours. Additional borane complex (0.084 mL) was added and reaction was heated at 60° C. for 1 hour. The reaction was cooled to ambient temperature and 0.3 mL of 1.25 M HCl in methanol was added. The quenched reaction was stirred 30 min and concentrated. The title compound was isolated after flash chromatography. ¹H NMR (400 MHz, pyridine-d₅, Temp=90° C.) δ ppm 8.05 (s, 1H), 7.88-7.82 (m, 2H), 7.47-7.38 (m, 4H), 7.36-7.29 (m, 2H), 7.26-7.15 (m, 5H), 4.85 (bs, 4H), 3.68-3.59 (m, 8H), 3.48-3.35 (m, 1H), 2.59 (t, J=7.0 Hz, 2H), 2.38-2.29 (m, 6H), 1.79-1.65 (m, 3H); MS (ESI(+)) m/e 485 (M+H)⁺.

Example 579 N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1H-pyrazol-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 5-bromo-N-(4-(2-cyclopentylacetamido)phenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 13.30 (bs, 0.25H), 12.87 (bs, 0.75H), 9.69 (s, 1H), 8.34-8.23 (m, 1H), 7.83-7.63 (m, 3H), 7.56-7.32 (m, 5H), 6.76-6.68 (m, 1H), 4.81-4.72 (m, 4H), 2.31-2.12 (m, 3H), 1.85-1.67 (m, 2H), 1.67-1.42 (m, 4H), 1.29-1.10 (m, 2H); MS (ESI(+)) m/e 430 (M+H)⁺.

Example 580 N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting pyridin-3-ylboronic acid for 1H-pyrazol-3-ylboronic acid and 5-bromo-N-(4-(2-cyclopentylacetamido)phenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (bs, 1H), 8.93-8.89 (m, 1H), 8.58 (dd, J=4.7, 1.6 Hz, 1H), 8.33 (s, 1H), 8.13-8.05 (m, 1H), 7.72 (bs, 1H), 7.71-7.64 (m, 1H), 7.54-7.44 (m, 6H), 4.81 (bs, 4H), 2.31-2.18 (m, 3H), 1.82-1.68 (m, 2H), 1.68-1.43 (m, 4H), 1.26-1.11 (m, 2H); MS (ESI(+)) m/e 441 (M+H)⁺.

Example 581 N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(1-methyl-1H-pyrazol-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole for 1H-pyrazol-3-ylboronic acid and 5-bromo-N-(4-(2-cyclopentylacetamido)phenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.69 (s, 1H), 8.27 (s, 1H), 8.14 (s, 1H), 7.88-7.85 (m, 1H), 7.55-7.40 (m, 6H), 7.36-7.30 (m, 1H), 4.77-4.69 (m, 4H), 3.86 (s, 3H), 2.31-2.16 (m, 3H), 1.81-1.68 (m, 2H), 1.68-1.42 (m, 4H), 1.28-1.12 (m, 2H); MS (ESI(+)) m/e 444 (M+H)⁺.

Example 582 N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-methoxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide

The title compound was prepared as described in Example 1C, substituting 2-methoxyethanamine for 3-phenylpropan-1-amine and 2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.69 (s, 1H), 8.56-8.49 (m, 1H), 8.31 (s, 1H), 7.84-7.77 (m, 2H), 7.50-7.40 (m, 5H), 4.78 (bs, 4H), 3.50-3.39 (m, 4H), 3.27 (s, 3H), 2.31-2.18 (m, 3H), 1.81-1.68 (m, 2H), 1.66-1.43 (m, 4H), 1.26-1.12 (m, 2H); MS (ESI(+)) m/e 465 (M+H)⁺.

Example 583 N²-{4-[(cyclopentylacetyl)amino]phenyl}-N⁵-(2-hydroxyethyl)-1,3-dihydro-2H-isoindole-2,5-dicarboxamide

The title compound was prepared as described in Example 1C, substituting 2-aminoethanol for 3-phenylpropan-1-amine and 2-({4-[(cyclopentylacetyl)amino]phenyl}carbamoyl)isoindoline-5-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, 1H), 8.51-8.40 (m, 1H), 8.31 (s, 1H), 7.86-7.75 (m, 2H), 7.51-7.36 (m, 5H), 4.78 (bs, 4H), 4.71 (t, J=5.6 Hz, 1H), 3.58-3.46 (m, 2H), 3.39-3.28 (m, 2H), 2.32-2.13 (m, 3H), 1.82-1.68 (m, 2H), 1.67-1.44 (m, 4H), 1.27-1.10 (m, 2H); MS (ESI(+)) m/e 451 (M+H)⁺.

Example 584 5-(aminomethyl)-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 276, substituting 5-cyano-N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide for 5-cyano-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.35 (bs, 1H), 7.99 (bs, 1H), 7.44-7.41 (m, 4H), 7.31-7.20 (m, 3H), 4.72 (bs, 4H), 3.81-3.68 (m, 2H), 2.29-2.25 (m, 3H), 1.80-1.68 (m, 2H), 1.66-1.48 (m, 6H), 1.29-1.14 (m, 2H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 605 N-[6-(benzoylamino)hexyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 605A tert-butyl 6-(isoindoline-2-carboxamido)hexylcarbamate

The title compound was prepared as described in Example 344A, substituting tert-butyl 6-aminohexylcarbamate for tert-butyl 5-aminoisoindoline-2-carboxylate.

Example 605B N-(6-aminohexyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting Boc-tert-butyl 6-(isoindoline-2-carboxamido)hexylcarbamate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 605C N-[6-(benzoylamino)hexyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(6-aminohexyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and benzoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.42 (t, J=5.35 Hz, 1H) 7.76-7.90 (m, 2H) 7.36-7.58 (m, 3H) 7.20-7.36 (m, 4H) 6.28 (t, J=5.55 Hz, 1H) 4.57 (s, 4H) 3.21-3.30 (m, 2H) 3.07 (q, J=6.74 Hz, 2H) 1.24-1.66 (m, 8H); (ESI(+)) m/e 366 (M+H)⁺.

TABLE 10 The following Examples were prepared as described in Example 1C, substituting N-(6-aminohexyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 606 N-{6-[(pyridin-3- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.98 (d, (ESI(+)) ylcarbonyl)amino]hexyl}- J = 1.36 Hz, 1H) 8.68 (dd, J = 4.75, 1.70 Hz, 1H) 8.62 m/e 367 1,3-dihydro-2H-isoindole-2- (t, J = 5.43 Hz, 1H) 8.12-8.21 (m, 1H) 7.48 (dd, (M + H)⁺ carboxamide J = 8.31, 5.26 Hz, 1H) 7.20-7.36 (m, 4H) 6.27 (t, J = 5.43 Hz, 1H) 4.57 (s, 4H) 3.23-3.29 (m, 2H) 2.99-3.13 (m, 2H) 1.25-1.60 (m, 9H) 619 N-(6-acetamidohexyl)- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.77 (s, 1H) (ESI(+)) 1,3-dihydro-2H-isoindole-2- 7.22-7.38 (m, 4H) 6.28 (t, J = 5.55 Hz, 1H) 4.57 (s, 4 m/e 304 carboxamide H) 2.93-3.14 (m, 4H) 1.77 (s, 3H) 1.31-1.61 (m, 4 (M + H)⁺ H) 1.20-1.31 (m, 4H) 655 N-(6-{[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) (methylsulfonyl)benzoyl]ami- Temp = 90° C.) δ ppm 1.33-1.40 (m, 4H), 1.45-1.63 m/e 444 no}hexyl)-1,3- (m, 4H), 3.11 (t, J = 7.02 Hz, 2H), 3.19 (s, 3H), 3.30 (M + H)⁺ dihydro-2H-isoindole-2- (t, J = 7.02 Hz, 2H), 4.59 (s, 4H), 7.24-7.33 (m, 4H), carboxamide 7.95-8.04 (m, 4H) 656 N-{6- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) [(ethoxyacetyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.15 (t, J = 7.02 Hz, 3H), 1.25- m/e 348 1,3-dihydro-2H-isoindole-2- 1.36 (m, 4H), 1.42-1.51 (m, 4H), 3.11 (q, J = 7.43 (M + H)⁺ carboxamide Hz, 4H), 3.50 (q, J = 7.02 Hz, 2H), 3.80 (s, 2H), 4.59 (s, 4H), 7.24-7.33 (m, 4H) 657 N-{6- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) [(cyclopentylcarbonyl)ami- Temp = 90° C.) δ ppm 1.25-1.35 (m, 5H), 1.38-1.55 m/e 358 no]hexyl}-1,3- (m, 6H), 1.56-1.67 (m, 4H), 1.68-1.81 (m, 2H), (M + H)⁺ dihydro-2H-isoindole-2- 3.00-3.13 (m, 4H), 4.59 (s, 4H), 7.20-7.37 (m, 4 carboxamide H) 658 N-{6-[(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) hydroxybenzoyl)amino] Temp = 90° C.) δ ppm 1.32-1.42 (m, 4H), 1.45-1.53 m/e 382 hexyl}-1,3-dihydro-2H- (m, 2H), 1.53-1.63 (m, 2H), 3.11 (t, 2H), 3.31 (t, (M + H)⁺ isoindole-2- J = 7.02 Hz, 2H), 4.58 (s, 4H), 6.83-6.90 (m, 2H), carboxamide 7.23-7.32 (m, 4H), 7.34-7.40 (m, 1H), 7.78 (dd, J = 7.78, 1.68 Hz, 1H) 659 N-{6-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) hydroxybenzoyl)amino] Temp = 90° C.) δ ppm 1.28-1.41 (m, 4H), 1.42-1.61 m/e 382 hexyl}-1,3-dihydro-2H- (m, 4H), 3.08-3.15 (m, 2H), 3.22-3.25 (m, 2H), (M + H)⁺ isoindole-2- 4.59 (s, 4H), 6.86-6.93 (m, 1H), 7.17-7.34 (m, 7 carboxamide H) 660 N-{6-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) hydroxybenzoyl)amino] Temp = 90° C.) δ ppm 1.30-1.38 (m, 4H), 1.44-1.60 m/e 382 hexyl}-1,3-dihydro-2H- (m, 4H), 3.09-3.13 (m, 2H), 3.20-3.25 (m, 2H), (M + H)⁺ isoindole-2- 4.59 (s, 4H), 6.75-6.83 (m, 2H), 7.23-7.32 (m, 4 carboxamide H), 7.65-7.71 (m, 2H) 661 N-{6-[(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) methoxybenzoyl)amino] Temp = 90° C.) δ ppm 1.29-1.43 (m, 4H), 1.45-1.61 m/e 396 hexyl}-1,3-dihydro-2H- (m, 4H), 3.08-3.15 (m, 2H), 3.30 (t, J = 7.02 Hz, 2 (M + H)⁺ isoindole-2- H), 3.89 (s, 3H), 4.58 (s, 4H), 6.99-7.04 (m, 1H), carboxamide 7.10 (d, J = 8.24 Hz, 1H), 7.24-7.32 (m, 4H), 7.41- 7.47 (m, 1H), 7.74 (dd, J = 7.63, 1.83 Hz, 1H) 662 N-{6-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) methoxybenzoyl)amino] Temp = 90° C.) δ ppm 1.30-1.41 (m, 4H), 1.44-1.62 m/e 396 hexyl}-1,3-dihydro-2H- (m, 4H), 3.09-3.14 (m, 2H), 3.26-3.31 (m, 2H), (M + H)⁺ isoindole-2- 3.80 (s, 3H), 4.58 (s, 4H), 7.03-7.07 (m, 1H), 7.24- carboxamide 7.41 (m, 7H) 663 N-{6-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) methoxybenzoyl)amino] Temp = 90° C.) δ ppm 1.31-1.39 (m, 4H), 1.49 (s, 4 m/e 396 hexyl}-1,3-dihydro-2H- H), 3.11 (t, J = 7.02 Hz, 2H), 3.26-3.28 (m, 2H), 3.80 (M + H)⁺ isoindole-2- (s, 3H), 4.58 (s, 4H), 6.92-6.97 (m, 2H), 7.24-7.32 carboxamide (m, 4H), 7.75-7.80 (m, 2H) 664 N-{6-[(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) fluorobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.27-1.42 (m, 4H), 1.43-1.64 m/e 384 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.11 (t, 2H), 3.28 (t, J = 7.02 Hz, 2H), 4.58 (M + H)⁺ carboxamide (s, 4H), 7.17-7.33 (m, 6H), 7.45-7.52 (m, 1H), 7.57-7.63 (m, 1H) 665 N-{6-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) fluorobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.32-1.41 (m, 4H), 1.44-1.61 m/e 384 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.11 (t, 2H), 3.28 (t, J = 7.02 Hz, 2H), 4.58 (M + H)⁺ carboxamide (s, 4H), 7.24-7.33 (m, 5H), 7.44-7.51 (m, 1H), 7.55-7.60 (m, 1H), 7.65 (d, J = 8.24 Hz, 1H) 666 N-{6-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) fluorobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.31-1.38 (m, 4H), 1.44-1.61 m/e 384 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.11 (t, J = 7.02 Hz, 2H), 3.26 (t, J = 7.02 Hz, (M + H)⁺ carboxamide 2H), 4.58 (s, 4H), 7.16-7.31 (m, 6H), 7.84-7.89 (m, 2H) 667 N-{6-[(2- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) chlorobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.30-1.42 (m, 4H), 1.45-1.63 m/e 400 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.12 (t, J = 7.02 Hz, 2H), 3.26-3.29 (m, 2 (M + H)⁺ carboxamide H), 4.59 (s, 4H), 7.24-7.32 (m, 4H), 7.33-7.45 (m, 4H) 668 N-{6-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) chlorobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.29-1.40 (m, 4H), 1.44-1.62 m/e 400 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.11 (t, 2H), 3.27 (t, 2H), 4.58 (s, 4H), (M + H)⁺ carboxamide 7.24-7.33 (m, 4H), 7.46 (t, J = 7.78 Hz, 1H), 7.51- 7.55 (m, 1H), 7.75 (dd, J = 7.63, 1.53 Hz, 1H), 7.82 (t, J = 1.68 Hz, 1H) 669 N-{6-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) chlorobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.28-1.40 (m, 4H), 1.44-1.62 m/e 400 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.11 (t, J = 7.02 Hz, 2H), 3.27 (t, 2H), 4.58 (M + H)⁺ carboxamide (s, 4H), 7.24-7.32 (m, 4H), 7.43-7.49 (m, 2H), 7.78-7.85 (m, 2H) 670 N-{6-[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) cyanobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.28-1.41 (m, 4H), 1.45-1.63 m/e 391 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.11 (t, 2H), 3.29 (t, J = 7.02 Hz, 2H), 4.58 (M + H)⁺ carboxamide (s, 4H), 7.24-7.32 (m, 4H), 7.65 (t, J = 7.78 Hz, 1H), 7.88-7.92 (m, 1H), 8.09-8.12 (m, 1H), 8.18 (t, 1H) 671 N-{6-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) cyanobenzoyl)amino]hexyl}- Temp = 90° C.) δ ppm 1.32-1.39 (m, 4H), 1.44-1.63 m/e 391 1,3-dihydro-2H-isoindole-2- (m, 4H), 3.11 (t, 2H), 3.29 (t, J = 7.02 Hz, 2H), 4.58 (M + H)⁺ carboxamide (s, 4H), 7.22-7.33 (m, 4H), 7.82-7.87 (m, 2H), 7.92-7.96 (m, 2H) 672 N-(6-{[3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) (dimethylamino)benzoyl]ami- Temp = 90° C.) δ ppm 1.30-1.38 (m, 4 H), 1.45-1.60 m/e 409 no}hexyl)-1,3- (m, 4 H), 2.96 (s, 6H), 3.11 (t, 2H), 3.27 (t, 2H), (M + H)⁺ dihydro-2H-isoindole-2- 4.59 (s, 4H), 6.93-7.00 (m, 1H), 7.17-7.21 (m, 1 carboxamide H), 7.24-7.33 (m, 6H) 673 N-(6-{[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) (dimethylamino)benzoyl]ami- Temp = 90° C.) δ ppm 1.31-1.37 (m, 4H), 1.43-1.58 m/e 409 no}hexyl)-1,3- (m, 4H), 2.95 (s, 6H), 3.11 (t, 2H), 3.24 (t, J = 7.02 (M + H)⁺ dihydro-2H-isoindole-2- Hz, 2H), 4.59 (s, 4H), 6.68-6.74 (m, 2H), 7.22- carboxamide 7.33 (m, 4H), 7.66-7.70 (m, 2H) 674 N-(6-{[3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) (trifluoromethyl)benzoyl]ami- Temp = 90° C.) δ ppm 1.32-1.41 (m, 4H), 1.46-1.62 m/e 434 no}hexyl)-1,3- (m, 4H), 3.09-3.14 (m, 2H), 3.30 (t, J = 7.02 Hz, 2 (M + H)⁺ dihydro-2H-isoindole-2- H), 4.58 (s, 4H), 7.24-7.33 (m, 4H), 7.68 (t, J = 7.78 carboxamide Hz, 1H), 7.83 (d, J = 7.63 Hz, 1H), 8.06-8.14 (m, 2H) 675 N-(6-{[4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) (trifluoromethyl)benzoyl]ami- Temp = 90° C.) δ ppm 1.32-1.41 (m, 4H), 1.45-1.62 m/e 434 no}hexyl)-1,3- (m, 4H), 3.11 (t, 2H), 3.30 (t, J = 7.17 Hz, 2H), 4.58 (M + H)⁺ dihydro-2H-isoindole-2- (s, 4H), 7.24-7.33 (m, 4H), 7.77 (d, J = 7.93 Hz, 2 carboxamide H), 7.98 (d, J = 7.93 Hz, 2H) 676 N-(6-{[3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) (trifluoromethoxy)benzoyl]ami- Temp = 90° C.) δ ppm 1.30-1.41 (m, 4H), 1.45-1.61 m/e 450 no}hexyl)-1,3- (m, 4H), 3.12 (t, J = 7.02 Hz, 2H), 3.29 (t, J = 7.17 Hz, (M + H)⁺ dihydro-2H-isoindole-2- 2H), 4.59 (s, 4H), 7.23-7.32 (m, 4H), 7.41-7.49 carboxamide (m, 1H), 7.58 (t, J = 7.93 Hz, 1H), 7.73 (s, 1H), 7.84 (d, J = 7.93 Hz, 1H) 677 N-{6-[(2,3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) dimethoxybenzoyl)ami- Temp = 90° C.) δ ppm 1.33-1.42 (m, 4H), 1.45-1.61 m/e 426 no]hexyl}-1,3-dihydro- (m, 4H), 3.12 (t, J = 7.02 Hz, 2H), 3.28 (t, J = 7.02 Hz, (M + H)⁺ 2H-isoindole-2- 2H), 3.79 (s, 3H), 3.83 (s, 3H), 4.58 (s, 4H), 7.06- carboxamide 7.20 (m, 3H), 7.24-7.32 (m, 4H) 678 N-{6-[(2,4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) dimethoxybenzoyl)ami- Temp = 90° C.) δ ppm 1.30-1.41 (m, 4H), 1.45-1.62 m/e 426 no]hexyl}-1,3-dihydro- (m, 4H), 3.11 (t, J = 7.02 Hz, 2H), 3.29 (t, J = 7.02 Hz, (M + H)⁺ 2H-isoindole-2- 2H), 3.81 (s, 3H), 3.90 (s, 3H), 4.58 (s, 4H), 6.56- carboxamide 6.63 (m, 2H), 7.22-7.33 (m, 4H), 7.78 (d, J = 8.54 Hz, 1H) 679 N-{6-[(2,5- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) dimethoxybenzoyl)ami- Temp = 90° C.) δ ppm 1.31-1.40 (m, 4H), 1.44-1.59 m/e 426 no]hexyl}-1,3-dihydro- (m, 4H), 3.12 (t, 2H), 3.30 (t, J = 6.87 Hz, 2H), 3.73 (M + H)⁺ 2H-isoindole-2- (s, 3H), 3.82-3.86 (m, 3H), 4.58 (s, 4H), 6.99-7.08 carboxamide (m, 2H), 7.23-7.34 (m, 5H) 680 N-{6- ¹H NMR (500 MHz, DMSO-d₆, Temp = 90° C.) δ 8.00 (ESI(+)) [(phenylacetyl)amino]hexyl}- (m, 1H), 7.28 (m, 8H), 7.20 (m, 1H), 6.27 (t, J = 5.5, m/e 380 1,3-dihydro-2H-isoindole-2- 1H), 4.57 (s, 4H), 3.04 (m, 4H), 1.40 (m, 4H), 1.27 (M + H)⁺ carboxamide (m, 4H) 681 N-(6-{[(3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (ESI(+)) fluorophenyl)acetyl]ami- Temp = 90° C.) δ ppm 1.22-1.33 (m, 4H), 1.36-1.53 m/e 398 no}hexyl)-1,3-dihydro- (m, 4H), 3.02-3.13 (m, 4H), 3.43 (s, 2H), 4.59 (s, 4 (M + H)⁺ 2H-isoindole-2- H), 6.93-7.12 (m, 3H), 7.23-7.34 (m, 5H) carboxamide 688 N-[6- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (s, 1H) (ESI(+)) (benzoylamino)hexyl]- 8.46 (d, J = 4.75 Hz, 1H) 8.41 (t, J = 5.43 Hz, 1H) 7.78- m/e 367 1,3-dihydro-2H- 7.86 (m, 2H) 7.40-7.55 (m, 3H) 7.38 (d, J = 5.09 (M + H)⁺ pyrrolo[3,4-c]pyridine- Hz, 1H) 6.36 (t, J = 5.43 Hz, 1H) 4.60 (d, J = 2.03 Hz, 2-carboxamide 4H) 3.21-3.29 (m, 2H) 3.00-3.13 (m, 2H) 1.25- 1.60 (m, 8H) 689 4-fluoro-N-{6-[(pyridin-3- ¹H NMR (500 MHz, DMSO-d₆, Temp = 90° C.) δ 9.02 (ESI(+)) ylcarbonyl)amino]hexyl}- (d, J = 2.2, 1H), 8.71 (m, 2H), 8.26 (dt, J = 7.9, 1.9, m/e 385 1,3-dihydro-2H-isoindole-2- 1H), 7.58 (ddd, J = 7.9, 4.8, 0.8, 1H), 7.34 (td, J = 7.8, (M + H)⁺ carboxamide 5.1, 1H), 7.16 (d, J = 7.5, 1H), 7.10 (t, J = 8.8, 1H), 6.39 (bs, 1H), 4.62 (s, 4H), 3.28 (m, 2H), 3.07 (m, 2H), 1.54 (m, 2H), 1.46 (m, 2H), 1.34 (m, 4H) 690 5-fluoro-N-{6-[(pyridin- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) 3-ylcarbonyl)amino]hexyl}- 8.99 (dd, J = 2.2, 0.9, 1H), 8.71 (m, 1H), 8.26 (m, m/e 385 1,3-dihydro-2H-isoindole-2- 1H), 7.58 (m, 1H), 7.32 (m, 1H), 7.08 (m, 2H), 4.58 (M + H)⁺ carboxamide (d, J = 2.5, 2H), 4.55 (m, 2H), 3.11 (t, J = 7.0, 2H), 1.47 (m, 11H) 691 5-methoxy-N-{6- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) [(pyridin-3- 9.01 (dd, J = 2.2, 0.9, 1H), 8.73 (dd, J = 5.0, 1.6, 1H), m/e 397 ylcarbonyl)amino]hexyl}- 8.33 (ddd, J = 7.9, 2.2, 1.6, 1H), 7.63 (ddd, J = 7.9, (M + H)⁺ 1,3-dihydro-2H-isoindole-2- 5.0, 0.9, 1H), 7.20 (m, 1H), 6.85 (m, 2H), 4.55 (m, carboxamide 2H), 4.50 (d, J = 2.4, 2H), 3.76 (s, 3H), 3.11 (t, J = 7.0, 2H), 1.58 (t, J = 7.0, 3H), 1.50 (t, J = 6.8, 2H), 1.36 (m, 5H) 692 N-{6-[(pyridin-3- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) ylcarbonyl)amino]hexyl}- 8.99 (dd, J = 2.2, 0.9, 1H), 8.71 (dd, J = 4.9, 1.6, 1H), m/e 435 5-(trifluoromethyl)- 8.27 (m, 1H), 7.58 (m, 4H), 4.66 (s, 4H), 3.12 (t, J = (M + H)⁺ 1,3-dihydro-2H-isoindole-2- 7.0, 2H), 1.54 (m, 5H), 1.37 (m, 5H) carboxamide 693 4-cyano-N-{6-[(pyridin- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) 3-ylcarbonyl)amino]hexyl}- 8.99 (m, 1H), 8.71 (dd, J = 5.0, 1.6, 1H), 8.28 (ddd, m/e 392 1,3-dihydro-2H-isoindole-2- J = 8.0, 2.3, 1.6, 1H), 7.67 (m, 2H), 7.59 (ddd, J = 7.9, (M + H)⁺ carboxamide 5.0, 0.9, 1H), 7.48 (t, J = 7.7, 1H), 4.75 (d, J = 2.2, 2H), 4.67 (m, 2H), 3.12 (t, J = 7.0, 2H), 1.56 (m, 5H), 1.37 (m, 5H) 694 5-methyl-N-{6- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) [(pyridin-3- 9.01 (m, 1H), 8.73 (dd, J = 5.0, 1.6, 1H), 8.32 (ddd, m/e 381 ylcarbonyl)amino]hexyl}- J = 7.9, 2.2, 1.6, 1H), 7.62 (ddd, J = 8.0, 5.0, 0.9, 1H), (M + H)⁺ 1,3-dihydro-2H-isoindole-2- 7.17 (d, J = 7.7, 1H), 7.08 (d, J = 7.8, 2H), 4.54 (bs, carboxamide 4H), 3.11 (t, J = 7.0, 2H), 2.31 (s, 3H), 1.56 (m, 5H), 1.37 (m, 5H) 695 4-chloro-N-{6- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) [(pyridin-3- 9.00 (dd, J = 2.2, 0.8, 1H), 8.71 (dd, J = 5.0, 1.6, 1H), m/e 401 ylcarbonyl)amino]hexyl}- 8.29 (ddd, J = 8.0, 2.2, 1.7, 1H), 7.60 (m, 1H), 7.30 (M + H)⁺ 1,3-dihydro-2H- (m, 3H), 4.63 (m, 4H), 3.32 (m, 2H), 3.12 (m, 2H), isoindole-2- 1.54 (m, 5H), 1.36 (m, 5H) carboxamide 696 5-cyano-N-{6-[(pyridin- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) 3-ylcarbonyl)amino]hexyl}- 8.98 (d, J = 1.7, 1H), 8.70 (dd, J = 4.9, 1.6, 1H), 8.24 m/e 392 1,3-dihydro-2H-isoindole-2- (m, 1H), 7.68 (m, 2H), 7.54 (m, 2H), 4.65 (m, 4H), (M + H)⁺ carboxamide 3.11 (m, 2H), 1.54 (m, 5H), 1.36 (m, 5H) 697 5-chloro-N-{6- ¹H NMR (400 MHz, DMSO-d₆_D₂O, Temp = 90° C.) δ (ESI(+)) [(pyridin-3- 8.99 (dd, J = 2.2, 0.7, 1H), 8.71 (dd, J = 5.0, 1.6, 1H), m/e 401 ylcarbonyl)amino]hexyl}- 8.27 (ddd, J = 8.0, 2.2, 1.7, 1H), 7.58 (m, 1H), 7.32 (M + H)⁺ 1,3-dihydro-2H- (m, 3H), 4.57 (dd, J = 8.2, 1.9, 4H), 3.11 (m, 2H), isoindole-2- 1.54 (m, 5H), 1.37 (m, 5H) carboxamide 698 N-{6-[(pyridin-2- ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.74 (t, J = 5.76 (ESI(+)) ylcarbonyl)amino]hexyl}- Hz, 1 H) 8.63 (d, J = 4.75 Hz, 1 H) 7.89-8.12 (m, 2 H) m/e 367 1,3-dihydro-2H- 7.50-7.65 (m, 1 H) 7.19-7.39 (m, 4 H) 6.26 (t, (M + H)⁺ isoindole-2- J = 5.43 Hz, 1 H) 4.57 (s, 4 H) 3.23-3.35 (m, 2 H) carboxamide 3.06 (q, J = 6.67 Hz, 2 H) 1.22-1.61 (m, 8 H)

Example 607 N-{4-[(cyclopentylacetyl)amino]phenyl}-5-(pyridin-4-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting pyridin-4-ylboronic acid for 1H-pyrazol-3-ylboronic acid and 5-bromo-N-(4-(2-cyclopentylacetamido)phenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, 1H), 8.69-8.61 (m, 2H), 8.33 (s, 1H), 7.82-7.69 (m, 4H), 7.54-7.41 (m, 5H), 4.81 (bs, 4H), 2.31-2.15 (m, 3H), 1.82-1.68 (m, 2H), 1.68-1.43 (m, 4H), 1.26-1.11 (m, 2H); MS (ESI(+)) m/e 441 (M+H)⁺.

Example 608 5-(hydroxymethyl)-N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-amino-N-isopentylbenzamide for 4-amino-N-propylbenzamide and isoindolin-5-ylmethanol hydrochloride for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (s, 1H), 8.24-8.17 (m, 1H), 7.79-7.72 (m, 2H), 7.68-7.61 (m, 2H), 7.37-7.21 (m, 3H), 5.19 (t, J=5.7 Hz, 1H), 4.76 (bs, 4H), 4.52 (d, J=5.7 Hz, 2H), 3.30-3.21 (m, 2H), 1.70-1.54 (m, 1H), 1.47-1.36 (m, 2H), 0.90 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 382 (M+H)⁺.

Example 609 N-{3-[(1-benzoylpiperidin-4-yl)oxy]propyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 609A tert-butyl 4-(3-(isoindoline-2-carboxamido)propoxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 344A, substituting tert-butyl 4-(3-aminopropoxy)piperidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate.

Example 609B N-(3-(piperidin-4-yloxy)propyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(3-(isoindoline-2-carboxamido)propoxy)piperidine-1-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 609C N-{3-[(1-benzoylpiperidin-4-yl)oxy]propyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(3-(piperidin-4-yloxy)propyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.21-7.50 (m, 9H) 6.27 (t, J=5.43 Hz, 1H) 4.57 (s, 4H) 3.40-3.58 (m, 6H) 3.07-3.21 (m, 2H) 1.74-1.93 (br m, 2H) 1.62-1.75 (m, 2H) 1.44 (br m, 2H); MS (ESI(+)) m/e 408 (M+H)⁺.

Example 610 N-(3-{[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]oxy}propyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting nicotinoyl chloride for acetyl chloride and N-(3-(piperidin-4-yloxy)propyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. 1H NMR (300 MHz, DMSO-d₆) δ ppm 8.51-8.70 (m, 2H) 7.75-7.88 (m, 1H) 7.46 (dd, J=7.73, 4.96 Hz, 1H) 7.20-7.38 (m, 3H) 6.28 (t, J=5.35 Hz, 1H) 4.57 (s, 4H) 3.83-4.01 (m, 1H) 3.40-3.63 (m, 6H) 3.16 (q, J=6.35 Hz, 2H) 1.35-1.95 (m, 7H); MS (ESI(+)) m/e 409 (M+H)⁺.

TABLE 11 The following Examples were essentially prepared as described in Example 1C, substituting N- (6-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-3-yl)isoindoline-2-carboxamide for 3-phenylpropan- 1-amine and the corresponding carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 614 N-[1′-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) 3-ylcarbonyl)- 8.70 (d, J = 2.6 Hz, 1H), 8.35 (s, 1H), 7.95 (dd, J = m/e 419 1′,2′,3′,6′-tetrahydro- 8.7, 2.6 Hz, 1H), 7.44 (d, J = 8.7 Hz, 1H), 7.40- (M + H)⁺ 2,4′-bipyridin-5-yl]- 7.24 (m, 4H), 6.54 (m, 1H), 4.79 (s, 4H), 4.19 (s, 1,3-dihydro-2H- 2H), 3.91 (t, J = 8.1 Hz, 1H), 3.72 (m, 5H), 3.40 (m, isoindole-2- 1H), 2.60 (s, 2H), 2.05 (m, 2H) carboxamide 615 N-{1′-[(2- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) methoxyethoxy)acetyl]- 8.69 (d, J = 2.6 Hz, 1H), 8.35 (s, 1H), 7.95 (dd, J = m/e 437 1′,2′,3′,6′-tetrahydro- 8.6, 2.6 Hz, 1H), 7.44 (d, J = 8.6 Hz, 1H), 7.38- (M + H)⁺ 2,4′-bipyridin-5-yl}- 7.27 (m, 4H), 6.54 (m, 1H), 4.79 (s, 4H), 4.19 (s, 1,3-dihydro-2H- 2H), 4.15 (m, 2H), 3.65 (t, J = 5.7 Hz, 2H), 3.60 (m, isoindole-2- 2H), 3.48 (m, 2H), 3.27 (s, 3H), 2.61 (m, 2H) carboxamide 711 N-[1′-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) 2-ylcarbonyl)- 8.69 (d, J = 2.6 Hz, 1H), 8.34 (s, 1H), 7.95 (dd, J = m/e 419 1′,2′,3′,6′-tetrahydro- 8.7, 2.6 Hz, 1H), 7.43 (d, J = 8.9 Hz, 1H), 7.39- (M + H)⁺ 2,4′-bipyridin-5-yl]- 7.23 (m, 4H), 6.54 (m, 1H), 4.79 (bs, 4H), 4.68 (dd, 1,3-dihydro-2H- J = 7.4, 5.8 Hz, 1H), 4.19 (bs, 2H), 3.88-3.62 (m, isoindole-2- 4H), 2.63 (m, 2H), 2.11 (m, 1H), 2.01 (m, 1H), 1.86 carboxamide (m, 2H) 712 N-[1′-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) pyran-4-ylcarbonyl)- 8.69 (dd, J = 2.6, 0.7 Hz, 1H), 8.34 (s, 1H), 7.95 (dd, m/e 433 1′,2′,3′,6′-tetrahydro- J = 8.6, 2.6 Hz, 1H), 7.43 (d, J = 8.9 Hz, 1H), 7.38- (M + H)⁺ 2,4′-bipyridin-5-yl]- 7.26 (m, 4H), 6.55 (m, 1H), 4.79 (s, 4H), 4.19 (m, 1,3-dihydro-2H- 2H), 3.86 (m, 2H), 3.70 (t, J = 5.7 Hz, 2H), 3.42 (td, isoindole-2- J = 11.4, 2.5 Hz, 2H), 2.92 (m, 1H), 2.60 (m, 2H), carboxamide 1.73-1.60 (m, 2H), 1.56 (m, 2H) 713 N-[1′-(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) ylcarbonyl)-1′,2′,3′,6′- 8.70 (d, J = 2.6 Hz, 1H), 8.35 (s, 1H), 7.96 (dd, J = m/e 435 tetrahydro-2,4′- 8.6, 2.6 Hz, 1H), 7.43 (d, J = 8.6 Hz, 1H), 7.38- (M + H)⁺ bipyridin-5-yl]-1,3- 7.26 (m, 4H), 6.54 (m, 1H), 4.79 (s, 4H), 4.37 (dd, dihydro-2H-isoindole- J = 9.1, 3.0 Hz, 1H), 4.20 (m, 2H), 3.83-3.61 (m, 2-carboxamide 7H), 3.52 (m, 1H), 2.61 (m, 2H) 714 N-{1′-[(1- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) methylpyrrolidin-3- 8.69 (dd, J = 2.6, 0.7 Hz, 1H), 8.34 (s, 1H), 7.95 (dd, m/e 432 yl)carbonyl]-1′,2′,3′,6′- J = 8.6, 2.6 Hz, 1H), 7.43 (d, J = 8.6 Hz, 1H), 7.38- (M + H)⁺ tetrahydro-2,4′- 7.26 (m, 4H), 6.54 (m, 1H), 4.79 (s, 4H), 4.16 (m, bipyridin-5-yl}-1,3- 2H), 3.68 (t, J = 5.7 Hz, 2H), 3.28 (m, 1H), 2.78 (t, dihydro-2H-isoindole- J = 8.6 Hz, 1H), 2.58 (m, 2H), 2.52 (m, 2H), 2.38 (q, 2-carboxamide J = 7.7 Hz, 1H), 2.24 (s, 3H), 2.98 (m, 2H) 715 N-{1′-[(1,1- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) dioxidotetrahydrothio- 8.70 (d, J = 2.6 Hz, 1H), 8.35 (s, 1H), 7.96 (dd, J = m/e 467 phen-3-yl)carbonyl]- 8.6, 2.6 Hz, 1H), 7.45 (d, J = 8.6 Hz, 1H), 7.38- (M + H)⁺ 1′,2′,3′,6′-tetrahydro- 7.27 (m, 4H), 6.55 (m, 1H), 4.79 (s, 4H), 4.21 (m, 2,4′-bipyridin-5-yl}- 2H), 3.79-3.65 (m, 3H), 3.36-3.13 (m, 3H), 3.08 1,3-dihydro-2H- (m, 1H), 2.63 (m, 2H), 2.37 (m, 1H), 2.14 (m, 1H) isoindole-2- carboxamide 758 N-[1′-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) methylpropanoyl)- 8.69 (d, J = 2.6 Hz, 1H), 8.34 (bs, 1H), 7.95 (dd, J = m/e 407 1′,2′,3′,6′-tetrahydro- 8.6, 2.6 Hz, 1H), 7.43(d, J = 8.6 Hz, 1H), 7.38- (M + H)⁺ 2,4′-bipyridin-5-yl]- 7.26 (m, 4H), 6.55 (m, 1H), 5.09 (s, 1H), 4.79 (s, 1,3-dihydro-2H- 4H), 4.32 (m, 2H), 3.93 (t, J = 5.7 Hz, 2H), 2.60 (m, isoindole-2- 2H), 1.37(s, 6H) carboxamide 800 N-[1′-(morpholin-4- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) ylacetyl)-1′,2′,3′,6′- 8.70 (d, J = 2.6 Hz, 1H), 8.34 (s, 1H), 7.95 (dd, J = m/e 448 tetrahydro-2,4′- 8.6, 2.6 Hz, 1H), 7.44 (d, J = 8.6 Hz, 1H), 7.38- (M + H)⁺ bipyridin-5-yl]-1,3- 7.27 (m, 4H), 6.54 (m, 1H), 4.79 (s, 4H), 4.20 (m, dihydro-2H-isoindole- 2H), 3.71 (t, J = 5.2 Hz, 2H), 3.58 (m, 4H), 3.21 (s, 2-carboxamide 2H), 2.48 (m, 2H), 2.45 (m, 4H) 1466 N-(4-{1-[(3R)- - ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ (ESI(+)) tetrahydrofuran-3- ppm 8.13 (s, 1H), 7.54 (m, 2H), 7.31 (m, 6H), 6.07 m/e 418 ylcarbonyl]-1,2,3,6- (m, 1H), 4.77 (s, 4H), 4.14 (m, 2H), 3.91 (t, J = 8.1 (M + H)⁺ tetrahydropyridin-4- Hz, 1H), 3.77-3.67 (m, 5H), 3.38 (m, 1H), 2.50 (m, yl}phenyl)-1,3- 2H), 2.02 (m, 2H) dihydro-2H-isoindole- 2-carboxamide 1467 N-(4-{1-[(3S)- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) tetrahydrofuran-3- 8.12 (s, 1H), 7.54 (m, 2H), 7.31 (m, 6H), 6.07 (m, m/e 418 ylcarbonyl]-1,2,3,6- 1H), 4.77 (s, 4H), 4.14 (m, 2H), 3.91 (t, J = 8.1 Hz, (M + H)⁺ tetrahydropyridin-4- 1H), 3.77-3.67 (m, 5H), 3.38 (m, 1H), 2.50 (m, yl}phenyl)-1,3- 2H), 2.05 (m, 2H) dihydro-2H-isoindole- 2-carboxamide 1468 N-(4-{1-[(1,1- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm (ESI(+)) dioxidotetrahydro-2H- 8.13 (s, 1H), 7.54 (m, 2H), 7.31 (m, 6H), 6.07 (m, m/e 480 thiopyran-4- 1H), 4.77 (s, 4H), 4.15 (m, 2H), 3.71 (t, J = 5.7 Hz, (M + H)⁺ yl)carbonyl]-1,2,3,6- 2H), 3.25-3.02 (m, 5H), 2.50 (m, 2H), 2.07 (m, 4H) tetrahydropyridin-4- yl}phenyl)-1,3- dihydro-2H-isoindole- 2-carboxamide

Example 611 N-(6-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 611A methyl 6-aminopyridazine-3-carboxylate

To a solution of 6-chloropyridazin-3-amine (32 g, 248 mmol), Et₃N (75 mL, 744 mmol) in MeOH (500 mL), Pd(dppf)Cl₂ (12 g, 16.4 mmol) was added and the mixture was heated at 60° C. overnight under CO atmosphere at 50 psi. After cooling to room temperature, the reaction mixture was filtered and the filtrate was concentrated under reduced pressure. The residue was washed with MeOH and the precipitate was dried by high vacuum to give the title compound as a solid.

Example 611B methyl 6-isocyanatopyridazine-3-carboxylate

To the solution of methyl 6-aminopyridazine-3-carboxylate (14 g, 91.5 mmol) in anhydrous toluene (700 mL) was added Et₃N (11.1, 109.8 mmol). A solution of triphosgene (27.2 g, 91.5 mmol) in anhydrous toluene was added slowly at 0° C. The reaction mixture was stirred for 2 hrs at room temperature and then heated at 90° C. for 5 hrs. After cooling to room temperature, toluene and water were added to the mixture, the mixture was separated and the organic layer was dried over anhydrous Na₂SO₄, concentrated under reduced pressure to give the title compound as a solid.

Example 611C methyl 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylate

To a solution of methyl 6-isocyanatopyridazine-3-carboxylate (5.26 g, 29.4 mmol) in THF (100 mL), a solution of isoindoline (5.24 g, 4.41 mmol) in THF (50 mL) was added at 0° C. The reaction mixture was stirred overnight at room temperature. The reaction mixture was filtered and the precipitate was washed with cold EtOAc and dried in high vacuum to give the title compound as a solid.

Example 611D 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylic acid

To a solution of methyl 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylate (3.7 g, 12.4 mmol) in MeOH (40 mL) and THF (40 mL), a solution of LiOH (0.7 g, 29.2 mmol) in water (10 mL) was added at room temperature. The reaction mixture was stirred overnight at room temperature. The reaction mixture was poured into water (100 mL), extracted with EtOAc (2×50 mL) and the aqueous layer was acidified by addition of 2 N HCl to pH 3 to give a precipitate. The precipitate was washed with water and dried in high vacuum to give the title compound.

Example 611E N-(6-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (S)-(tetrahydrofuran-3-yl)methamine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 9.94 (s, 1H), 9.12 (t, J=6.1 Hz, 1H), 8.31 (d, J=9.3 Hz, 1H), 8.11 (d, J=9.3 Hz, 1H), 7.41-7.28 (m, 4H), 4.89 (s, 4H), 3.80-3.55 (m, 3H), 3.50 (dd, J=8.5, 5.2 Hz, 1H), 3.37-3.31 (m, 2H), 2.63-2.51 (m, 1H), 2.01-1.85 (m, 1H), 1.71-1.55 (m, 1H); MS (ESI(+)) m/e 368 (M+H)⁺.

Example 612 N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting cyclopentylmethamine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 9.97 (s, 1H), 9.00 (t, J=6.1 Hz, 1H), 8.31 (d, J=9.3 Hz, 1H), 8.11 (d, J=9.3 Hz, 1H), 7.41-7.28 (m, 4H), 5.13-4.72 (m, 4H), 3.31-3.16 (m, 2H), 2.22 (p, J=7.3 Hz, 1H), 1.70-1.45 (m, 6H), 1.38-1.20 (m, 2H); MS (ESI(+)) m/e 366 (M+H)⁺.

Example 616 5-(hydroxymethyl)-N-(4-phenylbutyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1A, substituting (4-isocyanatobutyl)benzene for methyl 4-isocyanatobenzoate and isoindolin-5-ylmethanol hydrochloride for isoindoline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.32-7.12 (m, 8H), 6.32-6.24 (m, 1H), 5.16 (t, J=5.6 Hz, 1H), 4.54 (bs, 4H), 4.49 (d, J=5.7 Hz, 2H), 3.14-3.05 (m, 2H), 2.64-2.54 (m, 2H), 1.63-1.39 (m, 4H); MS (ESI(+)) m/e 325 (M+H)⁺.

Example 617 5-(hydroxymethyl)-N-[1-(3-methylbutyl)-1H-pyrazol-4-yl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 1-isopentyl-1H-pyrazol-4-amine dihydrochloride for 4-amino-N-propylbenzamide and isoindolin-5-ylmethanol hydrochloride for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.39 (s, 1H), 7.73 (s, 1H), 7.39 (s, 1H), 7.34-7.18 (m, 3H), 5.19 (t, J=5.6 Hz, 1H), 4.67 (bs, 4H), 4.51 (d, J=5.5 Hz, 2H), 4.04 (t, J=7.1 Hz, 2H), 1.71-1.55 (m, 2H), 1.55-1.33 (m, 1H), 0.89 (d, J=6.5 Hz, 6H); MS (ESI(+)) m/e 329 (M+H)⁺.

Example 618 N-{5-[(3-methylbutyl)carbamoyl]pyrazin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 618A ethyl 5-(isoindoline-2-carboxamido)pyrazine-2-carboxylate

The title compound was prepared as described in Example 344A, substituting ethyl 5-aminopyrazine-2-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate.

Example 618B 5-(isoindoline-2-carboxamido)pyrazine-2-carboxylic acid

The title compound was prepared as described in Example 1B, substituting ethyl 5-(isoindoline-2-carboxamido)pyrazine-2-carboxylate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 618C N-{5-[(3-methylbutyl)carbamoyl]pyrazin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 5-(isoindoline-2-carboxamido)pyrazine-2-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆, Temp=90° C.) δ ppm 9.34 (bs, 1H), 9.17 (d, J=1.4 Hz, 1H), 8.82 (d, J=1.4 Hz, 1H), 8.30-8.23 (m, 1H), 7.36-7.26 (m, 4H), 4.86 (bs, 4H), 3.37-3.30 (m, 2H), 1.69-1.58 (m, 1H), 1.50-1.44 (m, 2H), 0.92 (d, J=6.5 Hz, 6H); MS (ESI(+)) m/e 354 (M+H)⁺.

Example 621 N-(4-{(1E)-3-[benzyl(methyl)amino]prop-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 621A (E)-N-benzyl-N-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)prop-2-en-1-amine

In a 4 mL vial were mixed (E)-2-(3-chloroprop-1-enyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (0.195 ml, 0.988 mmol) and potassium carbonate (273 mg, 1.975 mmol) in anhydrous acetonitrile (2 ml). Benzylmethylamine (0.166 ml, 1.284 mmol) was added to this mixture, and the reaction was stirred vigorously overnight at room temperature. The reaction was diluted with ethyl acetate and washed with water and brine. The organic layer was dried with sodium sulfate, decanted, and concentrated to provide the title compound.

Example 621B N-(4-{(1E)-3-[benzyl(methyl)amino]prop-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting (E)-N-benzyl-N-methyl-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)prop-2-en-1-amine for 1H-pyrazol-3-ylboronic acid and N-(4-bromophenyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.12 (s, 1H), 7.52 (m, 2H), 7.37-7.18 (m, 11H), 6.48 (d, J=15.8 Hz, 1H), 6.18 (dt, J=15.8, 6.5 Hz, 1H), 4.77 (s, 4H), 3.53 (s, 2H), 3.15 (dd, J=6.5, 1.4 Hz, 2H), 2.18 (s, 3H); MS (ESI(+)) m/e 398 (M+H)⁺.

Example 622 N-[4-(4-phenoxypiperidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 622A 1-(4-nitrophenyl)-4-phenoxypiperidine

A solution of 1-fluoro-4-nitrobenzene (0.15 g, 1.063 mmol) and 4-phenoxypiperidine hydrochloride (0.250 g, 1.169 mmol) in dimethylformamide (2.126 ml) was treated with potassium carbonate (0.367 g, 2.66 mmol). The suspension was stirred at ambient temperature 2 hours, at 55° C. for 4 hours and at ambient temperature for 16 hours. The reaction was poured into water and the suspension was filtered and vacuum dried to provide the title compound.

Example 622B 4-(4-phenoxypiperidin-1-yl)aniline

The title compound was prepared as described in Example 272A, substituting 1-(4-nitrophenyl)-4-phenoxypiperidine for 4-nitro-N-propylbenzamide.

Example 622C N-[4-(4-phenoxypiperidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-(4-phenoxypiperidin-1-yl)aniline for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.11 (s, 1H), 7.42-7.24 (m, 8H), 7.02-6.86 (m, 5H), 4.74 (bs, 4H), 4.59-4.47 (m, 1H), 3.49-3.39 (m, 2H), 3.03-2.91 (m, 2H), 2.11-1.98 (m, 2H), 1.81-1.66 (m, 2H); MS (ESI(+)) m/e 414 (M+H)⁺.

Example 623 N-[4-(3-phenoxyazetidin-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 622, substituting 3-phenoxyazetidine for 4-phenoxypiperidine hydrochloride in Example 622A. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.06 (s, 1H), 7.44-7.25 (m, 8H), 7.03-6.93 (m, 1H), 6.92-6.85 (m, 2H), 6.47-6.40 (m, 2H), 5.19-5.08 (m, 1H), 4.73 (bs, 4H), 4.32-4.23 (m, 2H), 3.69 (dd, J=8.2, 4.2 Hz, 2H); MS (ESI(+)) m/e 386 (M+H)⁺.

Example 624 N-(4-{[benzyl(methyl)amino]methyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

A suspension of isoindoline (0.1 g, 0.839 mmol) and N-ethyl-N-isopropylpropan-2-amine (0.219 ml, 1.259 mmol) in acetonitrile (2.80 ml) was treated with N-methylpyrrolidine (2.80 ml). The solution was cooled to 0° C. and 1-(chloromethyl)-4-isocyanatobenzene (0.155 g, 0.923 mmol) was added. After stirring for 2 hours at 0° C., the reaction was treated with a solution of N-methyl-1-phenylmethanamine (0.102 g, 0.839 mmol) in 0.5 mL acetonitrile. The reaction was stirred at 0° C. for 5 minutes and at ambient temperature for 30 minutes. The reaction was treated with water and the mixture was stirred for 4 hours. The suspension was filtered and the solid collected was washed with water and dried under vacuum to provide the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.31 (s, 1H), 7.56-7.49 (m, 2H), 7.40-7.28 (m, 8H), 7.27-7.19 (m, 3H), 4.76 (bs, 4H), 3.47 (s, 2H), 3.43 (s, 2H), 2.06 (s, 3H); MS (ESI(+)) m/e 372 (M+H)⁺.

Example 625 5-fluoro-N-(4-{[(3R)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 410, substituting 5-fluoro-N-(4-{[tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide for N-(4-{[tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.39 (t, J=5.7 Hz, 1H), 7.81-7.73 (m, 2H), 7.69-7.62 (m, 2H), 7.40 (dd, J=8.4, 5.2 Hz, 1H), 7.24 (dd, J=9.1, 2.5 Hz, 1H), 7.15 (td, J=8.9, 2.5 Hz, 1H), 4.80-4.72 (m, 4H), 3.80-3.68 (m, 1H), 3.68-3.56 (m, 2H), 3.47 (dd, J=8.5, 5.2 Hz, 2H), 3.21 (dt, J=13.3, 5.9 Hz, 2H), 2.01-1.86 (m, 1H), 1.67-1.53 (m, 1H); MS (ESI(+)) m/e 384 (M+H)⁺.

Example 626 5-fluoro-N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 411, substituting 5-fluoro-N-(4-{[tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide for N-(4-{[tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.39 (t, J=5.7 Hz, 1H), 7.80-7.73 (m, 2H), 7.69-7.62 (m, 2H), 7.40 (dd, J=8.4, 5.2 Hz, 1H), 7.24 (dd, J=9.1, 2.5 Hz, 1H), 7.15 (td, J=8.9, 2.5 Hz, 1H), 4.80-4.73 (m, 4H), 3.80-3.56 (m, 3H), 3.47 (dd, J=8.5, 5.2 Hz, 1H), 3.24-3.13 (m, 2H), 2.01-1.86 (m, 1H), 1.67-1.53 (m, 1H); MS (ESI(+)) m/e 384 (M+H)⁺.

Example 636 N-[4-(1-benzyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 636A N-(4-ethynylphenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 1A, substituting 1-ethynyl-4-isocyanatobenzene for methyl 4-isocyanatobenzoate.

Example 636B N-[4-(1-benzyl-1H-1,2,3-triazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

A mixture of N-(4-ethynylphenyl)isoindoline-2-carboxamide (100 mg, 0.381 mmol), benzylamine (33.2 mg, 0.381 mmol), and sodium ascorbate (15 mg, 0.076 mmol) in methanol (1.9 ml) was treated with 1H-imidazole-1-sulfonyl azide hydrochloride (66.0 mg, 0.381 mmol), copper(II) sulfate pentahydrate (9.52 mg, 0.038 mmol) and triethylamine (63.8 μl, 0.457 mmol). Additional methanol (2 mL) was added and the vial was flushed with nitrogen and stirred for 2 days. The mixture was diluted with water and the resulting suspension was filtered with water washes to provide the title compound as a white solid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.51 (s, 1H), 8.45 (s, 1H), 7.73 (d, J=8.7 Hz, 2H), 7.65 (d, J=8.9 Hz, 2H), 7.49-7.24 (m, 9H), 5.63 (s, 2H), 4.78 (s, 4H), 1.11-1.00 (m, 1H); MS (ESI(+)) m/e 396 (M+H)⁺.

TABLE 12 The following Examples were essentially prepared as described in Example 636B, substituting the appropriate amine for benzylamine. Ex Name ¹H NMR MS 637 N-{4-[1-(3-methylbutyl)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.47 (s, 1H), 8.44 (ESI(+)) 1H-1,2,3-triazol-4- (s, 1H), 7.73 (d, J = 8.8 Hz, 2H), 7.65 (d, J = 8.8 m/e 376 yl]phenyl}-1,3-dihydro- Hz, 2H), 7.41-7.27 (m, 6H), 4.79 (s, 5H), 4.40 (t, (M + H)⁺ 2H-isoindole-2- J = 7.3 Hz, 2H), 1.77 (dd, J = 14.5, 7.0 Hz, 2H), carboxamide 1.52(dt, J = 13.4, 6.7 Hz, 1H), 0.93 (d, J = 6.6 Hz, 7H) 638 N-{4-[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.50 (s, 1H), 8.45 (ESI(+)) (tetrahydrofuran-3- (s, 1H), 7.73 (d, J = 8.9 Hz, 2H), 7.66 (d, J = 8.8 m/e 390 ylmethyl)-1H-1,2,3- Hz, 2H), 7.34 (ddd, J = 8.9, 4.2, 2.5 Hz, 4H), 4.79 (M + H)⁺ triazol-4-yl]phenyl}-1,3- (s, 4H), 4.39 (d, J = 7.5 Hz, 2H), 3.84-3.59 (m, dihydro-2H-isoindole-2- 3H), 3.51 (dd, J = 8.8, 5.4 Hz, 1H), 2.88-2.69 (m, carboxamide 1H), 2.04-1.86 (m, 1H), 1.73-1.55 (m, 1H) 639 N-(4-{1-[2-(2- ¹H NMR (400 MHz, DMSO-d₆) δ 8.46 (s, 2H), 7.72 (ESI(+)) oxopyrrolidin-1- (d, J = 8.8 Hz, 2H), 7.66 (d, J = 8.9 Hz, 2H), 7.37 m/e 417 yl)ethyl]-1H-1,2,3- (d, J = 5.5 Hz, 2H), 7.32 (dd, J = 5.6, 3.1 Hz, 2H), (M + H)⁺ triazol-4-yl}phenyl)-1,3- 4.79 (s, 4H), 4.53 (t, J = 5.9 Hz, 2H), 3.66 (t, J = dihydro-2H-isoindole-2- 5.9 Hz, 2H), 3.23 (t, J = 7.0 Hz, 2H), 2.15 (t, J = carboxamide 8.0 Hz, 2H), 1.94-1.76 (m, 2H) 640 N-{4-[1-(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.57 (s, 1H), 8.43 (ESI(+)) benzylpiperidin-4-yl)- (s, 1H), 7.73 (d, J = 8.7 Hz, 1H), 7.65 (d, J = 8.8 m/e 479 1H-1,2,3-triazol-4- Hz, 1H), 7.41-7.24 (m, 9H), 4.79 (s, 3H), 4.53 (td, (M + H)⁺ yl]phenyl}-1,3-dihydro- J = 10.6, 5.1 Hz, 1H), 3.54 (s, 2H), 2.98-2.88 (m, 2H-isoindole-2- 2H), 2.33-1.93 (m, 6H) carboxamide 641 N-{4-[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.50 (s, 1H), 8.45 (ESI(+)) phenylpropyl)-1H-1,2,3- (s, 1H), 7.74 (d, J = 8.7 Hz, 1H), 7.66 (d, J = 8.8 m/e 424 triazol-4-yl]phenyl}-1,3- Hz, 1H), 7.50-7.26 (m, 6H), 7.27-7.16 (m, 3H), (M + H)⁺ dihydro-2H-isoindole-2- 4.79 (s, 2H), 4.40 (t, J = 7.0 Hz, 2H), 2.62 (t, J = carboxamide 7.7 Hz, 2H), 2.29-2.07 (m, 1H) 642 N-(4-{1-[4-(morpholin- ¹H NMR (300 MHz, DMSO-d₆) δ 8.44 (s, 2H), 7.72 (ESI(+)) 4-yl)benzyl]-1H-1,2,3- (d, J = 8.7 Hz, 2H), 7.64 (d, J = 8.8 Hz, 2H), 7.42- m/e 481 triazol-4-yl}phenyl)-1,3- 7.19 (m, 6H), 6.94 (d, J = 8.7 Hz, 2H), 5.49 (s, 2H), (M + H)⁺ dihydro-2H-isoindole-2- 4.78 (s, 4H), 3.79-3.65 (m, 4H), 3.23-2.97 (m, carboxamide 4H) 643 N-[4-(1-isobutyl-1H- ¹H NMR (300 MHz, DMSO-d₆) δ 8.44 (s, 2H), 7.74 (ESI(+)) 1,2,3-triazol-4- (d, J = 8.7 Hz, 2H), 7.66 (d, J = 8.8 Hz, 2H), 7.41- m/e 362 yl)phenyl]-1,3-dihydro- 7.27 (m, 5H), 4.79 (s, 4H), 4.21 (d, J = 7.2 Hz, 2H), (M + H)⁺ 2H-isoindole-2- 2.29-2.06 (m, 1H), 0.90 (d, J = 6.7 Hz, 3H) carboxamide 644 N-{4-[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.46 (s, 1H), 8.44 (ESI(+)) (cyclopentylmethyl)-1H- (s, 1H), 7.73 (d, J = 8.7 Hz, 1H), 7.66 (d, J = 8.8 m/e 388 1,2,3-triazol-4- Hz, 1H), 7.41-7.28 (m, 4H), 4.79 (s, 2H), 4.31 (d, (M + H)⁺ yl]phenyl}-1,3-dihydro- J = 7.5 Hz, 1H), 3.31 (s, 2H), 2.40 (dt, J = 15.1, 7.4 2H-isoindole-2- Hz, 1H), 1.73-1.47 (m, 6H), 1.36-1.21 (m, 2H) carboxamide 645 N-{4-[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.46 (s, 1H), 8.45 (ESI(+)) methoxypropyl)-1H- (s, 1H), 7.73 (d, J = 8.8 Hz, 2H), 7.66 (d, J = 8.8 m/e 378 1,2,3-triazol-4- Hz, 2H), 7.42-7.26 (m, 4H), 4.79 (s, 4H), 4.43 (t, (M + H)⁺ yl]phenyl}-1,3-dihydro- J = 7.1 Hz, 2H), 3.38-3.32 (m, 1H), 3.25 (s, 3H), 2H-isoindole-2- 2.10 (p, J = 6.4 Hz, 2H) carboxamide

Example 646 N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide (50 mg, 0.128 mmol) and methanol (10 ml) were added to 5% Pd—C, wet (10.00 mg, 0.094 mmol) in a 50 ml pressure bottle and stirred for 16 hours at 30 psi and room temperature. The mixture was filtered through a nylon membrane and concentrated. Chromatography provided the title compound. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.35 (s, 1H), 7.49-7.40 (m, 3H), 7.13 (m, 2H), 4.79 (m, 4H), 4.56 (m, 1H), 4.05 (m, 1H), 3.12 (m, 1H), 2.90 (m, 1H), 2.71 (m, 1H), 2.57 (m, 1H), 1.79 (m, 2H), 1.55-1.30 (m, 2H), 1.02 (m, 6H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 647 N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 646, substituting N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide for N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.27 (s, 1H), 7.47 (m, 2H), 7.39-7.28 (m, 4H), 7.12 (m, 2H), 4.75 (bs, 4H), 4.47 (m, 1H), 4.24-4.09 (m, 2H), 3.90 (m, 1H), 3.57 (m, 2H), 3.47 (t, J=4.7 Hz, 2H), 3.26 (s, 3H), 3.06 (m, 1H), 2.70 (m, 1H), 2.62 (m, 1H), 1.77 (m, 2H), 1.57 (m, 1H), 1.42 (m, 1H); MS (ESI(+)) m/e 438 (M+H)⁺.

Example 648 N-{5-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]pyridin-2-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 646, substituting N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-3,4′-bipyridin-6-yl]-1,3-dihydro-2H-isoindole-2-carboxamide for N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.81 (s, 1H), 8.16 (d, J=2.4 Hz, 1H), 7.85 (d, J=8.6 Hz, 1H), 7.63 (dd, J=8.7, 2.4 Hz, 1H), 7.39-7.25 (m, 4H), 4.80 (s, 4H), 4.56 (d, J=13.1 Hz, 1H), 4.08 (d, J=12.3 Hz, 1H), 3.88 (m, 1H), 3.72 (m, 3H), 3.38 (m, 1H), 3.11 (m, 1H), 2.78 (dd, J=11.9, 9.2 Hz, 1H), 2.63 (m, 1H), 2.03 (m, 2H), 1.80 (t, J=15.4 Hz, 2H), 1.51 (m, 2H); MS (ESI(+)) m/e 421 (M+H)⁺.

Example 651 N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 651A N-(6-chloropyridin-3-yl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 1A, substituting 2-chloro-5-isocyanatopyridine for methyl 4-isocyanatobenzoate and 2,3-dihydro-1H-pyrrolo[3,4-c]pyridine for isoindoline.

Example 651B tert-butyl 4-(5-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridin-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate

The title compound was prepared as described in Example 280, substituting tert-butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for 1H-pyrazol-3-ylboronic acid and N-(6-chloropyridin-3-yl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide.

Example 651C N-(6-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-3-yl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(5-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridin-2-yl)-5,6-dihydropyridine-1(2H)-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 651D N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(6-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-3-yl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and isobutanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (501 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.73 (d, J=2.6 Hz, 1H), 8.64 (s, 1H), 8.52 (m, 2H), 7.99 (dd, J=8.6, 2.6 Hz, 1H), 7.49 (d, J=8.7 Hz, 1H), 7.44 (d, J=5.0 Hz, 1H), 6.60 (m, 1H), 4.88 (bs, 2H), 4.85 (d, J=2.3 Hz, 2H), 4.22 (m, 2H), 3.73 (t, J=5.7 Hz, 2H), 2.96 (m, 1H), 2.63 (m, 2H), 1.08 (d, J=6.7 Hz, 6H); MS (ESI(+)) m/e 392 (M+H)⁺.

TABLE 13 The following Examples were essentially prepared as described in Example 1C, substituting N-(6-(1,2,3,6-tetrahydropyridin-4-yl)pyridin-3-yl)-1H-pyrrolo [3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and the corresponding carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 652 N-(1′-benzoyl-1′,2′,3′,6′- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e tetrahydro-2,4′-bipyridin- ppm 8.70 (d, J = 2.6 Hz, 1H), 8.60 (s, 1H), 426 (M + H)⁺ 5-yl)-1,3-dihydro-2H- 8.49 (d, J = 5.0 Hz, 1H), 8.44 (s, 1H), 7.96 pyrrolo[3,4-c]pyridine-2- (dd, J = 8.6, 2.6 Hz, 1H), 7.49-7.37 (m, 7H), carboxamide 6.56 (bs, 1H), 4.83 (m, 4H), 4.22 (m, 2H), 3.64 (m, 2H), 2.64 (m, 2H) 653 N-[1′-(tetrahydrofuran-3- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e ylcarbonyl)-1′,2′,3′,6′- ppm 8.70 (s, 1H), 8.60 (bs, 1H), 8.49 (dd, J = 420 (M + H)⁺ tetrahydro-2,4′-bipyridin- 8.6, 2.7 Hz , 1H), 8.43 (s, 1H), 7.95 (d, J = 2.7 5-yl]-1,3-dihydro-2H- Hz, 1H), 7.45 (d, J = 8.6, 1H), 7.40 (d, J = 2.7 pyrrolo[3,4-c]pyridine-2- Hz, 1H) 6.56 (bs, 1H), 4.78 (m, 4H), 4.20 (m, carboxamide 2H), 3.92 (m, 1H), 3.72 (m, 4H), 3.40 (m, 1H), 2.60 (m, 2H), 2.05 (m, 3H) 654 N-{1′-[(2- ¹H NMR (501 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e methoxyethoxy)acetyl]- ppm 8.69 (d, J = 2.6 Hz, 1H), 8.59 (s, 1H), 438 (M + H)⁺ 1′,2′,3′,6′-tetrahydro-2,4′- 8.49 (d, J = 5.0 Hz, 1H), 8.47 (m, 1H), 7.95 bipyridin-5-yl}-1,3- (dd, J = 8.6, 2.6 Hz, 1H), 7.45 (d, J = 8.7 Hz, dihydro-2H-pyrrolo[3,4- 1H), 7.40 (d, J = 5.1 Hz, 1H), 6.55 (bs, 1H), c]pyridine-2- 4.84 (bs, 2H), 4.81 (bs, 2H), 4.19 (s, 2H), 4.14 carboxamide (m, 2H), 3.65 (m, 2H), 3.60 (m, 2H), 3.48 (m, 2H), 3.26 (s, 3H), 2.60 (m, 2H) 700 N-[1′-(tetrahydrofuran-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e ylcarbonyl)-1′,2′,3′,6′- ppm 8.69 (dd, J = 8.7, 2.6 Hz, in), 8.59 (s, 420 (M + H)⁺ tetrahydro-2,4′-bipyridin- 1H), 8.48 (d, J = 8.7, 1H), 8.42 (bs, 1H), 7.94 5-yl]-1,3-dihydro-2H- (dd, J = 8.7, 2.6 Hz, 1H), 7.44 (m, 1H), 7.39 pyrrolo[3,4-c]pyridine-2- (d, J = 5.1, 1H) 6.55 (m, 1H), 4.82 (m, 4H), carboxamide 4.68 (dd, J = 7.5, 5.8 Hz, 1H), 4.19 (bs, 2H), 3.88-3.62 (m, 4H), 2.60 (m, 2H), 2.10 (m, 1H), 2.01 (m, 1H), 1.87 (m, 2H) 701 N-[1′-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e pyran-4-ylcarbonyl)- ppm 8.69 (d, J = 2.5 Hz, 1H), 8.59 (s, 1H), 434 (M + H)⁺ 1′,2′,3′,6′-tetrahydro-2,4′- 8.48 (d, J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.94 bipyridin-5-yl]-1,3- (dd, J = 8.7, 2.6 Hz, 1H), 7.44 (d, J = 8.6 Hz, dihydro-2H-pyrrolo[3,4- 1H), 7.39 (d, J = 4.9 Hz, 1H), 6.55 (m, 1H), c]pyridine-2- 4.82 (m, 4H), 4.18 (bs, 2H), 3.85 (m, 2H), 3.70 carboxamide (t, J = 5.8 Hz, 2H), 3.42 (td, J = 11.4, 2.5 Hz, 2H), 2.92 (m, 1H), 2.60 (bs, 2H), 1.66 (m, 2H), 1.57 (m, 2H) 702 N-[1′-(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e ylcarbonyl)-1′,2′,3′,6′- ppm 8.69 (dd, J = 2.7, 0.5 Hz, 1H), 8.59 (s, 436 (M + H)⁺ tetrahydro-2,4′-bipyridin- 1H), 8.48 (d, J = 5.0 Hz, 1H), 8.43 (bs, 1H), 5-yl]-1,3-dihydro-2H- 7.94 (dd, J = 8.7, 2.6 Hz, 1H), 7.43 (m, 1H), pyrrolo[3,4-c]pyridine-2- 7.39 (m, 1H), 6.54 (m, 1H), 4.82 (m, 4H), 4.37 carboxamide (dd, J = 9.2, 2.9 Hz, 1H), 4.18 (bs, 2H), 3.82- 3.61 (m, 7H), 3.52 (m, 1H), 2.61 (s, 2H) 703 N-{1′-[(1,1- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e dioxidotetrahydrothiophen- ppm 8.69 (d, J = 2.4 Hz, 1H), 8.59 (s, 1H), 468 (M + H)⁺ 3-yl)carbonyl]- 8.48 (d, J = 5.0 Hz, 1H), 8.43 (s, 1H), 7.95 1′,2′,3′,6′-tetrahydro-2,4′- (dd, J = 8.7, 2.6 Hz, 1H), 7.45 (d, J = 8.7 Hz, bipyridin-5-yl}-1,3- 1H), 7.39 (d, J = 4.9 Hz, 1H), 6.55 (m, 1H), dihydro-2H-pyrrolo[3,4- 4.82 (m, 4H), 4.21 (s, 2H), 3.85-3.65 (m, c]pyridine-2- 3H), 3.35-3.13 (m, 3H), 3.06 (m, 1H), 2.63 carboxamide (bs, 2H), 2.37 (m, 1H), 2.13 (m, 1H) 704 N-[1′-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) m/e methylpropanoyl)- ppm 8.68 (s, 1H), 8.59 (s, 1H), 8.48 (d, J = 4.8 408 (M + H)⁺ 1′,2′,3′,6′-tetrahydro-2,4′- Hz, 1H), 8.41 (s, 1H), 7.94 (m, 1H), 7.43 (d, bipyridin-5-yl]-1,3- J = 8.6 Hz, 1H), 7.39 (d, J = 4.7 Hz, 1H), 6.55 dihydro-2H-pyrrolo[3,4- (m, 1H), 5.09 (s, 1H), 4.82 (m, 4H), 4.32 (bs, c]pyridine-2- 2H), 3.92 (bs, 2H), 2.59 (bs, 2H), 1.37 (s, 6H) carboxamide

Example 699 N-{4-[1-(pyridin-2-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting picolinoyl chloride for acetyl chloride and N-[4-(piperidin-4-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (d, J=4.76 Hz, 1H) 7.83-7.97 (m, 1H) 7.38-7.57 (m, 2H) 7.18-7.40 (m, 4H) 6.27 (t, J=5.55 Hz, 1H) 4.56 (s, 4H) 4.47 (d, J=13.09 Hz, 1H) 3.59 (d, J=13.88 Hz, 1H) 3.00-3.16 (m, 3H) 2.92-3.01 (m, 1H) 2.68-2.81 (m, 1H) 1.77 (d, J=12.69 Hz, 1H) 0.97-1.64 (m, 11H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 718 N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 718A benzyl(tetrahydrofuran-3-yl)methylcarbamate

Racemic (tetrahydrofuran-3-yl)methanamine (3.84 g, 38.0 mmol) and diisopropylethylamine (13.26 ml, 76 mmol), were dissolved in dichloromethane (100 ml) and cooled to 0° C. The mixture was treated dropwise via an addition funnel with benzyl carbonochloridate (6.19 ml, 41.8 mmol) dissolved in 30 ml dichlormethane. After the addition the cooling bath was removed and the homogeneous solution was stirred at ambient temperature overnight. The reaction mixture was partitioned between water and ethyl acetate and the separated aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with brine, dried over magnesium sulfate, filtered and concentrated. Chromatography provided the title compound.

Example 718B (S)-benzyl(tetrahydrofuran-3-yl)methylcarbamate

A racemic mixture of benzyl(tetrahydrofuran-3-yl)methylcarbamate was dissolved in tetrahydrofuran and separated by liquid chromatography with a Chiralpak IC 2.5 cm ID×25 cm, 20 micron column, eluting with hexane/tetrahydrofuran/isopropanol (85/10/5), to provide (R)-benzyl(tetrahydrofuran-3-yl)methylcarbamate and (S)-benzyl(tetrahydrofuran-3-yl)methylcarbamate.

Example 718C (S)-(tetrahydrofuran-3-yl)methanamine

(R)-Benzyl(tetrahydrofuran-3-yl)methylcarbamate (8.9 g, 37.8 mmol) and ethanol (160 ml) were added to 20% wet palladium (II) hydroxide (0.890 g, 6.34 mmol) in a 250 mL stainless steel pressure bottle and stirred for 40 minutes at 30 psi and room temperature. The mixture was filtered through a nylon filter and acidified with 4N HCl in dioxane (5 eq). Concentration and drying provided the title compound.

Example 718D N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (S)-(tetrahydrofuran-3-yl)methanamine for 3-phenylpropan-1-amine and 4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)benzoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.64 (s, 2H), 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.38 (t, J=5.7 Hz, 1H), 7.81-7.74 (m, 2H), 7.69-7.62 (m, 2H), 7.44 (d, J=5.1 Hz, 1H), 4.86-4.79 (m, 4H), 3.80-3.66 (m, 2H), 3.67-3.56 (m, 1H), 3.47 (dd, J=8.5, 5.3 Hz, 1H), 3.21 (dt, J=13.2, 5.8 Hz, 1H), 2.01-1.86 (m, 1H), 1.67-1.53 (m, 1H); MS (ESI(+)) m/e 367 (M+H)⁺.

Example 720 N-(7-oxo-7-{[(3R)-tetrahydrofuran-3-ylmethyl]amino}heptyl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 720A methyl 7-(isoindoline-2-carboxamido)heptanoate

The title compound was prepared as described in Example 344A, substituting methyl 7-aminoheptanoate for tert-butyl 5-aminoisoindoline-2-carboxylate.

Example 720B 7-(isoindoline-2-carboxamido)heptanoic acid

The title compound was prepared as described in Example 1B, substituting methyl 7-(isoindoline-2-carboxamido)heptanoate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 720C N-(7-oxo-7-{[(3R)-tetrahydrofuran-3-ylmethyl]amino}heptyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (R)-(tetrahydrofuran-3-yl)methanamine for 3-phenylpropan-1-amine and 7-(isoindoline-2-carboxamido)heptanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.85 (t, J=5.76 Hz, 1H) 7.20-7.37 (m, 4H) 6.26 (t, J=5.59 Hz, 1H) 4.57 (s, 4H) 3.49-3.79 (m, 3H) 3.35 (dd, J=8.48, 5.43 Hz, 1H) 2.94-3.15 (m, 4H) 2.18-2.38 (m, 1H) 2.05 (t, J=7.29 Hz, 2H) 1.79-1.98 (m, 1H) 1.35-1.60 (m, 7H) 1.17-1.35 (m, 2H); MS (ESI(+)) m/e 374 (M+H)⁺.

Example 721 N-{7-oxo-7-[(tetrahydro-2H-pyran-4-ylmethyl)amino]heptyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (tetrahydro-2H-pyran-4-yl)methanamine for 3-phenylpropan-1-amine and 7-(isoindoline-2-carboxamido)heptanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.76 (t, J=5.75 Hz, 1H) 7.20-7.40 (m, 4H) 6.26 (t, J=5.55 Hz, 1H) 4.57 (s, 4H) 3.82 (dd, J=11.10, 2.78 Hz, 2H) 3.14-3.29 (m, 2H) 3.05 (q, J=6.74 Hz, 2H) 2.92 (t, J=6.15 Hz, 2H) 2.06 (t, J=7.54 Hz, 2H) 1.33-1.65 (m, 9H) 1.19-1.34 (m, 2H) 0.98-1.22 (m, 2H); MS (ESI(+)) m/e 388 (M+H)⁺.

Example 722 N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 722A tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)butyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 344, substituting tert-butyl 4-(4-aminobutyl)piperidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate and substituting 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for isoindoline in Example 344A.

Example 722B N-(4-(piperidin-4-yl)butyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)butyl)piperidine-1-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 722C N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(piperidin-4-yl)butyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and benzoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (500 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.54 (s, 1H) 8.45 (d, J=5.04 Hz, 1H) 7.38-7.46 (m, 3H) 7.28-7.37 (m, 3H) 6.09 (s, 1H) 4.62 (dd, J=9.08, 1.60 Hz, 4H) 3.07-3.15 (m, 2H) 2.79-2.94 (m, 2H) 1.61-1.75 (m, 2H) 1.41-1.58 (m, 3H) 1.20-1.40 (m, 4H) 0.99-1.17 (m, 2H); MS (ESI(+)) m/e 407 (M+H)⁺.

TABLE 14 The following Examples were essentially prepared as described in Example 722C, substituting an appropriate carboxylic acid for benzoic acid. Ex Name ¹H NMR MS 757 N-{4-[1-(2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.55 (s, 1H) 8.46 (ESI(+)) chlorobenzoyl)piperidin- (d, J = 5.16 Hz, 1H) 7.25-7.57 (m, 5H) 6.36 (t, m/e 441 4-yl]butyl}-1,3- J = 5.55 Hz, 1H) 4.60 (s, 2H) 4.60 (s, 2H) 4.43-4.54 (M + H)⁺ dihydro-2H- (m, 1H) 3.13-3.28 (m, 1H) 2.85-3.12 (m, 3H) 2.74 pyrrolo[3,4-c]pyridine- (t, J = 12.10 Hz, 1H) 1.76 (d, J = 13.09 Hz, 1H) 0.86- 2-carboxamide 1.67 (m, 10H) 1350 N-{4-[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.63 (s, (ESI(+)) (tetrahydrofuran-2- 1H), 8.53 (d, J = 5.3 Hz, 1H), 7.52 (d, J = 5.3 Hz, 1H), m/e 415 ylacetyl)piperidin-4- 6.13-5.96 (m, 1H), 4.67 (s, 1H), 4.09 (p, J = 6.6 Hz, (M + H)⁺ yl]butyl}-1,3-dihydro- 2H), 3.73 (q, J = 7.2 Hz, 5H), 3.10 (t, J = 7.0 Hz, 2H), 2H-pyrrolo[3,4- 2.82-2.55 (m, 3H), 2.35 (dd, J = 14.8, 6.5 Hz, 2H), c]pyridine-2- 2.04-1.92 (m, 2H), 1.79 (tt, J = 12.8, 6.3 Hz, 2H), carboxamide 1.66 (d, J = 12.9 Hz, 2H), 1.54-1.42 (m, 3H), 1.39- 1.29 (m, 2H), 1.24 (dd, J = 14.3, 5.9 Hz, 2H), 1.06- 0.90 (m, 2H) 1351 N-(4-{1-[(1,1- 1H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) dioxidotetrahydrothiophen-3- 1H), 8.55 (d, J = 5.2 Hz, 1H), 7.55 (d, J = 5.3 Hz, 1H), m/e 449 yl)carbonyl]piperidin- 6.08 (s, 1H), 4.68 (s, 5H), 3.70-3.58 (m, 2H), 3.22- (M + H)⁺ 4-yl}butyl)-1,3- 3.15 (m, 3H), 3.15-3.00 (m, 3H), 2.29 (td, J = 12.8, dihydro-2H- 7.0 Hz, 2H), 2.08 (ddd, J = 17.0, 13.4, 8.8 Hz, 2H), pyrrolo[3,4-c]pyridine- 1.69 (d, J = 12.9 Hz, 2H), 1.50 (ddt, J = 21.4, 14.3, 7.3 2-carboxamide Hz, 3H), 1.40-1.21 (m, 4H), 1.03 (d, J = 11.6 Hz, 2H) 1352 N-{4-[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.62 (s, (ESI(+)) (tetrahydrofuran-3- 1H), 8.52 (d, J = 5.3 Hz, 1H), 7.51 (d, J = 5.1 Hz, 1H), m/e 415 ylacetyl)piperidin-4- 6.13-5.95 (m, 1H), 4.65 (d, J = 7.1 Hz, 4H), 3.83- (M + H)⁺ yl]butyl}-1,3-dihydro- 3.75 (m, 1H), 3.70 (td, J = 8.0, 5.3 Hz, 1H), 3.57 (dd, 2H-pyrrolo[3,4- J = 24.8, 17.4 Hz, 2H), 3.28-3.14 (m, 3H), 3.10 (t, J = c]pyridine-2- 7.0 Hz, 2H), 2.40-2.26 (m, 3H), 1.99 (dt, J = 12.8, carboxamide 7.6 Hz, 2H), 1.66 (d, J = 10.4 Hz, 3H), 1.55-1.40 (m, 3H), 1.36-1.16 (m, 3H), 0.99 (d, J = 9.4 Hz, 3H) 1353 N-{4-[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (cyclohexylcarbonyl)pi- 1H), 8.54 (d, J = 5.2 Hz, 1H), 7.54 (d, J = 5.3 Hz, 1H), m/e 413 peridin-4-yl]butyl}- 6.08 (s, 1H), 4.68 (s, 4H), 4.17-3.95 (m, 4H), 3.10 (t, (M + H)⁺ 1,3-dihydro-2H- J = 7.0 Hz, 2H), 2.78-2.53 (m, 3H), 1.72-1.62 (m, pyrrolo[3,4-c]pyridine- 5H), 1.57 (d, J = 14.8 Hz, 3H), 1.46 (dd, J = 14.3, 7.3 2-carboxamide Hz, 3H), 1.39-1.13 (m, 6H), 1.03-0.91 (m, 2H) 1354 N-(4-{1-[(4,4- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.61 (s, (ESI(+)) difluorocyclohexyl)car- 1H), 8.52 (d, J = 5.2 Hz, 1H), 7.49 (d, J = 5.2 Hz, 1H), m/e 449 bonyl]piperidin-4- 6.17-5.91 (m, 1H), 4.66 (s, 4H), 4.17-3.95 (m, 3H), (M + H)⁺ yl}butyl)-1,3-dihydro- 3.10 (t, J = 7.0 Hz, 2H), 2.84-2.68 (m, 3H), 2.09- 2H-pyrrolo[3,4- 1.96 (m, 2H), 1.93-1.77 (m, 2H), 1.65 (dd, J = 27.2, c]pyridine-2- 12.8 Hz, 6H), 1.56-1.40 (m, 2H), 1.41-1.20 (m, carboxamide 4H), 1.06-0.92 (m, 2H) 1355 N-{4-[1-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.62 (s, (ESI(+)) methylpropanoyl)pi- 1H), 8.53 (d, J = 5.2 Hz, 1H), 7.51 (d, J = 5.2 Hz, 1H), m/e 389 peridin-4-yl]butyl}-1,3- 6.18-5.92 (m, 1H), 4.67 (s, 4H), 4.52-4.43 (m, 2H), (M + H)⁺ dihydro-2H- 3.10 (t, J = 7.0 Hz, 2H), 2.82-2.70 (m, 2H), 1.70- pyrrolo[3,4-c]pyridine- 1.62 (m, 2H), 1.56-1.42 (m, 4H), 1.32 (s, 8H), 1.28 2-carboxamide (d, J = 13.3 Hz, 2H), 1.08-1.02 (m, 2H) 1356 N-(4-{1-[(2R)- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.63 (s, (ESI(+)) tetrahydrofuran-2- 1H), 8.53 (d, J = 5.2 Hz, 1H), 7.53 (d, J = 5.2 Hz, 1H), m/e 401 ylcarbonyl]piperidin- 6.08 (s, 1H), 4.67 (s, 4H), 4.58 (dd, J = 7.5, 5.6 Hz, (M + H)⁺ 4-yl}butyl)-1,3- 2H), 4.20-4.05 (m, 3H), 3.83-3.62 (m, 3H), 3.10 (t, dihydro-2H- J = 7.0 Hz, 2H), 2.76 (bs, 2H), 2.11-1.99 (m, 1H), pyrrolo[3,4-c]pyridine- 2.00-1.75 (m, 3H), 1.71-1.63 (m, 2H), 1.46 (dd, J = 2-carboxamide 14.2, 7.2 Hz, 2H), 1.37-1.19 (m, 2H), 1.10-0.92 (m, 2H) 1357 N-(4-{1-[(2S)- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.62 (s, (ESI(+)) tetrahydrofuran-2- 1H), 8.53 (d, J = 5.2 Hz, 1H), 7.51 (d, J = 5.2 Hz, 1H), m/e 401 ylcarbonyl]piperidin- 6.07 (s, 1H), 4.67 (s, 4H), 4.58 (dd, J = 7.5, 5.6 Hz, (M + H)⁺ 4-yl}butyl)-1,3- 1H), 3.77 (q, J = 7.2 Hz, 2H), 3.82-3.67 (m, 3H), dihydro-2H- 3.10 (t, J = 7.0 Hz, 2H), 2.75 (bs, 1H), 2.11-1.99 (m, pyrrolo[3,4-c]pyridine- 1H), 2.00-1.75 (m, 3H), 1.71-1.62 (m, 2H), 1.53- 2-carboxamide 1.21 (m, 7H), 1.08-0.92 (m, 2H) 1358 N-(4-{1-[(2- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.62 (s, (ESI(+)) methoxyethoxy)acetyl] 1H), 8.53 (d, J = 5.2 Hz, 1H), 7.51 (d, J = 5.2 Hz, 1H), m/e 419 piperidin-4-yl}butyl)- 6.15-5.99 (m, 1H), 4.67 (s, 4H), 4.58 (dd, J = 7.5, (M + H)⁺ 1,3-dihydro-2H- 5.6 Hz, 2H), 3.77 (q, J = 7.2 Hz, 2H), 3.82-3.67 (m, pyrrolo[3,4-c]pyridine- 3H), 3.10 (t, J = 7.0 Hz, 2H), 2.75 (bs, 1H), 2.11- 2-carboxamide 1.99 (m, 1H), 1.95 (ddd, J = 17.4, 9.9, 6.6 Hz, 1H), 1.88-1.77 (m, 1H), 1.71-1.62 (m, 2H), 1.46 (dd, J = 14.4, 7.4 Hz, 3H), 1.37-1.19 (m, 4H), 1.08-0.92 (m, 2H) 1359 N-{4-[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (tetrahydrofuran-3- 4H), 8.54 (d, J = 5.3 Hz, 1H), 7.55 (d, J = 5.3 Hz, 1H), m/e 401 ylcarbonyl)piperidin- 6.08 (s, 1H), 4.68 (s, 4H), 3.85 (t, J = 8.1 Hz, 1H), (M + H)⁺ 4-yl]butyl}-1,3- 3.73-3.58 (m, 2H), 3.33-3.22 (m, 2H), 3.10 (t, J = dihydro-2H- 7.0 Hz, 2H), 1.99 (dd, J = 14.3, 7.1 Hz, 3H), 1.68 (d, pyrrolo[3,4-c]pyridine- J = 12.7 Hz, 2H), 1.55-1.41 (m, 3H), 1.33 (dt, J = 2-carboxamide 13.8, 6.4 Hz, 2H), 1.24 (dd, J = 13.4, 6.3 Hz, 2H), 0.99 (dd, J = 24.0, 12.4 Hz, 2H) 1360 N-(4-{1-[(propan-2- ¹H NMR (400 MHz, DMSO; Temp = 90° C.) δ 8.63 (s, (ESI(+)) yloxy)acetyl]piperidin- 4H), 8.53 (d, J = 5.3 Hz, 1H), 7.53 (d, J = 5.2 Hz, 1H), m/e 403 4-yl}butyl)-1,3- 6.09 (s, 1H), 4.66 (d, J = 7.5 Hz, 5H), 3.60 (dt, J = (M + H)⁺ dihydro-2H- 12.2, 6.1 Hz, 2H), 3.10 (t, J = 7.0 Hz, 2H), 1.67 (d, J = pyrrolo[3,4-c]pyridine- 13.1 Hz, 2H), 1.54-1.41 (m, 3H), 1.33 (dd, J = 15.9, 2-carboxamide 7.1 Hz, 2H), 1.24 (dd, J = 14.3, 5.7 Hz, 3H), 1.10 (d, J = 6.1 Hz, 6H), 1.02 (d, J = 11.2 Hz, 2H) 1361 N-{4-[1- ¹H NMR (400 MHz, DMSO, Temp = 90° ) δ 8.63 (s, (ESI(+)) (cyclopropylacetyl)pi- 4H), 8.54 (d, J = 5.3 Hz, 1H), 7.54 (d, J = 5.3 Hz, 1H), m/e 385 peridin-4-yl]butyl}-1,3- 6.13-6.00 (m, 1H), 4.67 (s, 4H), 3.10 (t, J = 7.0 Hz, (M + H)⁺ dihydro-2H- 2H), 2.22 (d, J = 6.6 Hz, 2H), 1.63 (t, J = 21.9 Hz, pyrrolo[3,4-c]pyridine- 2H), 1.47 (dt, J = 14.1, 7.0 Hz, 3H), 1.38-1.28 (m, 2-carboxamide 2H), 1.24 (dd, J = 14.3, 5.8 Hz, 2H), 1.07-0.85 (m, 4H), 0.47-0.39 (m, 2H), 0.15-0.05 (m, 2H) 1362 N-{4-[1-(4,4,4- ¹H NMR (400 MHz, DMSO Temp = 90° ) δ 8.63 (s, (ESI(+)) trifluorobutanoyl)pi- 4H), 8.53 (d, J = 5.3 Hz, 1H), 7.52 (d, J = 5.3 Hz, 1H), m/e 427 peridin-4-yl]butyl}-1,3- 6.07 (s, 1H), 4.67 (s, 4H), 3.10 (t, J = 7.0 Hz, 2H), (M + H)⁺ dihydro-2H- 1.67 (d, J = 13.3 Hz, 2H), 1.47 (dt, J = 14.3, 7.1 Hz, pyrrolo[3,4-c]pyridine- 3H), 1.38-1.29 (m, 4H), 1.25 (dt, J = 13.6, 6.8 Hz, 2-carboxamide 3H), 1.03 (s, 3H)

Example 753 N-{4-[5-(morpholin-4-ylmethyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 753A N-(4-(5-(chloromethyl)-1,2,4-oxadiazol-3-yl)phenyl)isoindoline-2-carboxamide

To a 25 mL round-bottomed flask containing (Z)—N-(4-(N′-hydroxycarbamimidoyl)phenyl)isoindoline-2-carboxamide (1.5 g, 5.06 mmol) in acetone (5 ml) was added potassium carbonate (7.00 g, 50.6 mmol) in a single portion. The reaction mixture was cooled to 0° C. and 2-chloroacetyl chloride (3.22 ml, 40.5 mmol) was added slowly. The resulting mixture was warmed to room temperature and stirred for two hours. The solvent was removed and the solid was triturated with water and then filtered with water washes. The dried solid was dissolved in DMF, heated to 100° C. and stirred for two hours. Work-up with water and dichlormethane followed by chromatography provided the title compound.

Example 753B N-{4-[5-(morpholin-4-ylmethyl)-1,2,4-oxadiazol-3-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

To a 20 mL vial was added N-(4-(5-(chloromethyl)-1,2,4-oxadiazol-3-yl)phenyl)isoindoline-2-carboxamide (50 mg, 0.141 mmol) and morpholine (36.8 mg, 0.423 mmol) in DMF (470 μl). The mixture was heated to 50° C. for 30 minutes, cooled, and diluted with 2 mL methanol. Chromatography provided the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ 8.69 (s, 1H), 7.92 (d, J=8.8 Hz, 2H), 7.80 (d, J=8.9 Hz, 2H), 7.35 (ddd, J=8.8, 3.9, 2.4 Hz, 4H), 4.80 (s, 4H), 3.95 (s, 2H), 3.68-3.48 (m, 4H), 2.62-2.51 (m, 5H); MS (ESI(+)) m/e 406 (M+H)⁺.

Example 754 N-(4-{5-[(4-methylpiperazin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 753B, substituting 1-methylpiperazine for morpholine. ¹H NMR (300 MHz, DMSO-d₆) δ 8.69 (s, 1H), 7.91 (d, J=8.8 Hz, 3H), 7.80 (d, J=8.8 Hz, 3H), 7.45-7.23 (m, 5H), 4.80 (s, 5H), 3.93 (s, 2H), 2.65-2.51 (m, 75H), 2.34 (s, 5H), 2.15 (s, 4H); MS (ESI(+)) m/e 419 (M+H)⁺.

Example 755 N-[4-{(5-[(3-methylbutyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 753B, substituting 3-methylbutan-1-amine for morpholine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.68 (s, 1H), 7.91 (d, J=8.8 Hz, 2H), 7.79 (d, J=8.8 Hz, 2H), 7.35 (tdd, J=8.9, 5.4, 3.4 Hz, 4H), 4.80 (s, 4H), 4.02 (s, 2H), 2.66-2.53 (m, 1H), 2.43-2.30 (m, 1H), 1.63 (dt, J=13.4, 6.7 Hz, 1H), 1.32 (dd, J=14.4, 7.0 Hz, 2H), 0.86 (d, J=6.5 Hz, 6H); MS (ESI(+)) m/e 406 (M+H)⁺.

Example 756 N-(4-{5-[(4-hydroxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 753B, substituting piperidin-4-ol for morpholine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.68 (s, 1H), 7.91 (d, J=8.8 Hz, 2H), 7.79 (d, J=8.8 Hz, 2H), 7.45-7.25 (m, 4H), 4.80 (s, 4H), 4.56 (d, J=4.2 Hz, 1H), 3.91 (s, 2H), 3.45 (dd, J=8.7, 4.3 Hz, 1H), 3.17 (d, J=5.2 Hz, 1H), 2.76 (dd, J=10.6, 5.0 Hz, 2H), 2.42-2.18 (m, 3H), 1.72 (d, J=8.9 Hz, 2H), 1.43 (dt, J=18.5, 6.4 Hz, 2H); MS (ESI(+)) m/e 420 (M+H)⁺.

Example 787 N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}-2-oxoethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 787A N-benzyl-N-(3-morpholinopropyl)-2-(4-nitrophenyl)acetamide

The title compound was prepared as described in Example 1C, substituting N-benzyl-3-morpholinopropan-1-amine for 3-phenylpropan-1-amine and 2-(4-nitrophenyl)acetic acid for 4-(isoindoline-2-carboxamido)benzoic acid.

Example 787B 2-(4-aminophenyl)-N-benzyl-N-(3-morpholinopropyl)acetamide

The title compound was prepared as described in Example 272A, substituting N-benzyl-N-(3-morpholinopropyl)-2-(4-nitrophenyl)acetamide for 4-nitro-N-propylbenzamide.

Example 787C N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}-2-oxoethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 2-(4-aminophenyl)-N-benzyl-N-(3-morpholinopropyl)acetamide for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.05 (bs, 1H), 7.47 (d, J=8.5 Hz, 2H), 7.37-7.17 (m, 9H), 7.15-7.08 (m, 2H), 4.76 (s, 4H), 4.56 (bs, 2H), 3.77-3.55 (m, 2H), 3.56-3.50 (m, 4H), 3.30 (t, J=7.3 Hz, 2H), 2.33-2.24 (m, 4H), 2.21 (t, J=6.8 Hz, 2H), 1.60 (p, J=7.1 Hz, 2H); MS (ESI(+)) m/e 513 (M+H)⁺.

Example 788 N-[4-(3-{benzyl[3-(morpholin-4-yl)propyl]amino}-3-oxopropyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 787, substituting 3-(4-nitrophenyl)propanoic acid for 2-(4-nitrophenyl)acetic acid in Example 787A. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 7.99 (bs, 1H), 7.48-7.39 (m, 2H), 7.37-7.19 (m, 7H), 7.19-7.13 (m, 2H), 7.13-7.00 (m, 2H), 4.76 (s, 4H), 4.53 (s, 2H), 3.56-3.45 (m, 4H), 3.31-3.23 (m, 2H), 2.87-2.78 (m, 2H), 2.72-2.57 (m, 2H), 2.29-2.22 (m, 4H), 2.20 (t, J=6.8 Hz, 2H), 1.63-1.54 (m, 2H); MS (ESI(+)) m/e 527 (M+H)⁺.

Example 795 N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting tetrahydro-2H-pyran-4-ylmethamine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 9.98 (s, 1H), 9.03 (t, J=6.2 Hz, 1H), 8.31 (d, J=9.3 Hz, 1H), 8.10 (d, J=9.3 Hz, 1H), 7.41-7.28 (m, 4H), 5.03-4.67 (m, 4H), 3.89-3.79 (m, 2H), 3.29-3.11 (m, 4H), 2.01-1.78 (m, 1H), 1.63-1.53 (m, 2H), 1.30-1.12 (m, 2H); MS (ESI(+)) m/e 382 (M+H)⁺.

Example 797 N-[4-(6-bromo-2-oxoquinolin-1(2H)-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 797A tert-butyl 4-(6-bromo-2-oxoquinolin-1(2H)-yl)butylcarbamate

To a solution of 6-bromoquinolin-2(1H)-one (430 mg, 1.91 mmol) in tetrahydrofuran (8 ml) was added sodium bis(trimethylsilyl)amide (2.1 ml, 2.08 mmol). After 15 minutes, 4-(boc-amino)butyl bromide (403 mg, 1.6 mmol) was added. The solution was stirred for 15 hours, concentrated and purified by flash chromatography to provide the title compound.

Example 797B 1-(4-aminobutyl)-6-bromoquinolin-2(1H)-one

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(6-bromo-2-oxoquinolin-1(2H)-yl)butylcarbamate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 797C N-[4-(6-bromo-2-oxoquinolin-1(2H)-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 1-(4-aminobutyl)-6-bromoquinolin-2(1H)-one for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (400 MHz, CDCl₃) δ ppm 7.67 (d, J=2.2 Hz, 2H), 7.61 (d, J=2.3 Hz, 1H), 7.60 (d, J=2.3 Hz, 1H), 7.57 (d, J=9.6 Hz, 2H), 7.28 (s, 1H), 7.24 (s, 1H), 6.70 (d, J=9.5 Hz, 2H), 4.76 (t, J=5.7 Hz, 2H), 4.70 (s, 4H), 4.29 (m, 2H), 3.42 (m, 2H), 1.79 (m, 2H), 1.69 (m, 2H); MS (ESI(+)) m/e 440.1 (M+H).

Example 798 N-{4-[6-(3-acetylphenyl)-2-oxoquinolin-1(2H)-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 3-acetylphenyl boronic acid for 1H-pyrazol-3-ylboronic acid and N-[4-(6-bromo-2-oxoquinolin-1(2H)-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, CDCl₃) δ ppm 8.20 (t, J=1.5 Hz, 1H), 7.94 (d, J=7.7 Hz, 1H), 7.80 (m, 3H), 7.75 (d, J=9.5 Hz, 2H), 7.56 (t, J=7.7 Hz, 1H), 7.49 (d, J=9.4 Hz, 2H), 7.24 (s, 1H), 6.75 (t, J=9.4 Hz, 2H), 4.82 (t, J=5.4 Hz, 1H), 4.72 (s, 4H), 4.37 (m, 2H), 3.45 (m, 2H), 2.66 (s, 3H), 1.88 (m, 2H), 1.74 (m, 2H); MS (ESI(+)) m/e 480.3 (M+H).

Example 804 5-(hydroxymethyl)-N-(3-phenylpropyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 3-phenylpropan-1-amine for 4-amino-N-propylbenzamide and isoindolin-5-ylmethanol hydrochloride for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.30-7.14 (m, 8H), 6.30 (t, J=5.5 Hz, 1H), 5.16 (t, J=5.5 Hz, 1H), 4.55 (bs, 4H), 4.49 (d, J=4.9 Hz, 2H), 3.16-3.05 (m, 2H), 2.64-2.56 (m, 2H), 1.76 (p, J=7.4 Hz, 2H); MS (ESI(+)) m/e 311 (M+H)⁺.

Example 805 N-(2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazol-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 805A methyl 2-(4-(pyridin-3-yl)benzylamino)thiazole-5-carboxylate

In a 250 mL round-bottomed flask was added 4-(pyridin-3-yl)benzaldehyde (4 g, 21.83 mmol), methyl 2-aminothiazole-5-carboxylate (3.45 g, 21.83 mmol), and acetic acid (0.375 ml, 6.55 mmol) in toluene (109 ml). The mixture was heated at reflux under Dean-Stark conditions for 3 hours, cooled, concentrated and redissolved in methanol. The mixture was cooled to 0° C. and sodium borohydride (1.322 g, 34.9 mmol) was carefully added. The mixture was warmed to room temperature and the resulting suspension was filtered with water washes to provide the title compound after drying.

Example 805B 2-(4-fluorobenzyl)(4-(pyridin-3-yl)benzyl)amino)thiazole-5-carboxylic acid

In a 250 mL round-bottomed flask was added methyl 2-(4-(pyridin-3-yl)benzylamino)thiazole-5-carboxylate (3 g, 9.22 mmol) and 1-(bromomethyl)-4-fluorobenzene (1.264 ml, 10.14 mmol) in dimethylformamide (46.1 ml). The mixture was cooled to 0° C., sodium hydride (0.738 g, 18.44 mmol) was added carefully; and the mixture was warmed to room temperature. After the mixture was stirred for about 30 minutes, it was found to be predominantly carboxylic acid. 1 N NaOH was added to complete the conversion; and a water work up followed by chromatography provided the title compound.

Example 805C N-(4-fluorobenzyl)-5-isocyanato-N-(4-(pyridin-3-yl)benzyl)thiazol-2-amine

To a 50 mL round-bottomed flask was added 2-((4-fluorobenzyl)(4-(pyridin-3-yl)benzyl)amino)thiazole-5-carboxylic acid (850 mg, 2.026 mmol) in dichloromethane (10.100 ml) and the solution was cooled to 0° C. Oxalyl chloride (0.266 ml, 3.04 mmol) and dimethylformamide (0.016 ml, 0.203 mmol) were added and some bubbling occurred. The solution was warmed to room temperature and stirred for 1 hour. The mixture was cooled to 0° C., and trimethylsilyl azide (0.538 ml, 4.05 mmol) was added. The mixture was warmed to room temperature, stirred for 30 minutes and concentrated under vacuum. Toluene (5 ml) was added and the mixture was heated to 95° C. for 2.5 hours. The toluene was removed and the resulting solid was triturated/sonicated with ether and filtered with ether washes to provide the title compound.

Example 805D N-(2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazol-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1A, substituting N-(4-fluorobenzyl)-5-isocyanato-N-(4-(pyridin-3-yl)benzyl)thiazol-2-amine for methyl 4-isocyanatobenzoate and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for isoindoline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.27 (s, 1H), 8.99 (d, J=2.1 Hz, 1H), 8.76 (s, 1H), 8.71-8.56 (m, 2H), 8.29 (d, J=7.8 Hz, 1H), 7.81-7.56 (m, 5H), 7.51-7.27 (m, 5H), 7.27-7.06 (m, 2H), 6.86 (s, 1H), 4.80 (d, J=3.6 Hz, 4H), 4.72 (d, J=7.7 Hz, 4H); MS (ESI(+)) m/e 537 (M+H)⁺.

Example 806 N-[4-(2-benzyl-1,3-thiazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 806A 4-(2-benzylthiazol-4-yl)aniline

2-Bromo-1-(4-nitrophenyl)ethanone (0.5 g, 2.049 mmol) and 2-phenylethanethioamide (0.310 g, 2.049 mmol) were combined in ethanol (10 ml) in a 20 mL microwave reaction vessel and heated at 140° C. for 15 minutes. The solution was transferred to a 250 mL round bottom flask where it immediately solidified. The material was diluted with an additional ethanol (10 ml) and was heated at reflux with stirring until the solids were dissolved. Water (5.0 ml, 278 mmol), and hydrochloric acid (1 ml, 12.00 mmol) were added. Iron (0.625 g, 11.19 mmol) was added and the mixture was heated at reflux for 2 hours. The mixture was allowed to cool and 5 mL NH₄OH was added. The material was filtered through a pad of diatomaceous earth and the pad was washed with 50 mL of ethyl acetate. The filtrate was washed with 100 mL of water and the aqueous phase was extracted with an additional 50 mL of ethyl acetate. The combined organic fractions were dried over sodium sulfate, filtered, and the solvent was removed under reduced pressure. The material was re-dissolved in 50 mL of ethyl acetate and filtered through a ¼-inch pad of silica gel. The pad was washed with an additional 50 mL of ethyl acetate and the combined filtrate was concentrated to provide the title compound.

Example 806B N-[4-(2-benzyl-1,3-thiazol-4-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-(2-benzylthiazol-4-yl)aniline for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (400 MHz, CDCl₃) δ ppm 7.79 (d, J=8.7 Hz, 2H), 7.48 (d, J=8.7 Hz, 2H), 7.30 (s, 1H), 7.29 (d, J=3.8 Hz, 2H), 7.26 (m, 5H), 7.20 (d, J=3.7 Hz, 2H), 6.29 (s, 1H), 4.80 (s, 4H), 4.32 (s, 2H); MS (ESI(+)) m/e 412 (M+H).

Example 807 N-(7-{benzyl[3-(morpholin-4-yl)propyl]amino}-7-oxoheptyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-benzyl-3-morpholinopropan-1-amine for 3-phenylpropan-1-amine and 7-(isoindoline-2-carboxamido)heptanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.41-7.13 (m, 9H), 6.32-6.22 (m, 1H), 4.59-4.48 (m, 6H), 3.58-3.47 (m, 4H), 3.27-3.20 (m, 2H), 3.11-2.98 (m, 2H), 2.44-2.36 (m, 1H), 2.31-2.23 (m, 5H), 2.23-2.12 (m, 2H), 1.70-1.17 (m, 10H); MS (ESI(+)) m/e 507 (M+H)⁺.

Example 808 N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 808A N-isopentyl-4-nitrobenzenesulfonamide

4-Nitrobenzene-1-sulfonyl chloride (1.5 g, 6.57 mmol) was dissolved in dichloromethane (30 ml) and cooled to 0° C. followed by addition of diisopropylethylamine (2.293 ml, 13.13 mmol). 3-Methylbutan-1-amine (0.926 ml, 7.88 mmol) was dissolved in 5 ml dichloromethane and added via syringe. After the addition, the mixture was allowed to warm to room temperature for 3 hours. The solution was diluted with aqueous sodium bicarbonate and extracted twice with dichloromethane. The organics were combined, dried over magnesium sulfate, filtered and concentrated. Chromatography provided the title compound.

Example 808B 4-amino-N-isopentylbenzenesulfonamide

The title compound was prepared as described in Example 272A, substituting N-isopentyl-4-nitrobenzenesulfonamide for 4-nitro-N-propylbenzamide.

Example 808C N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-amino-N-isopentylbenzenesulfonamide for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.75 (s, 1H), 7.82-7.74 (m, 2H), 7.70-7.64 (m, 2H), 7.41-7.27 (m, 5H), 4.80 (s, 4H), 2.77-2.67 (m, 2H), 1.64-1.47 (m, 1H), 1.30-1.19 (m, 2H), 0.79 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 388 (M+H)⁺.

Example 839 N-(5-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}pyridin-2-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (S)-benzyl(tetrahydrofuran-3-yl)methylcarbamate for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)nicotinic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (500 MHz, DMSO-d₆) δ ppm 9.27 (s, 1H), 8.74 (d, J=2.1 Hz, 1H), 8.60 (t, J=5.7 Hz, 1H), 8.14 (dd, J=8.8, 2.4 Hz, 1H), 8.00 (d, J=8.7 Hz, 1H), 7.41-7.27 (m, 4H), 4.89 (m, 4H), 3.75 (m, 1H), 3.69 (m, 1H), 3.62 (m, 1H), 3.48 (dd, J=8.5, 5.3 Hz, 1H), 3.25 (m, 2H), 2.48 (m, 1H), 1.95 (m, 1H), 1.61 (m, 1H); MS (ESI(+)) m/e 367 (M+H).

Example 871 N-[4-(4-{benzyl[3-(morpholin-4-yl)propyl]amino}-4-oxobutyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 787, substituting 3-(4-nitrophenyl)butanoic acid for 2-(4-nitrophenyl)acetic acid in Example 787A. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.29-8.21 (m, 1H), 7.51-7.41 (m, 2H), 7.40-7.13 (m, 9H), 7.11-6.98 (m, 2H), 4.75 (s, 4H), 4.57-4.47 (m, 2H), 3.60-3.44 (m, 4H), 3.27-3.13 (m, 2H), 2.60-2.53 (m, 1H), 2.48-2.34 (m, 2H), 2.33-2.11 (m, 7H), 1.90-1.71 (m, 2H), 1.66-1.51 (m, 2H); MS (ESI(+)) m/e 541 (M+H)⁺.

Example 872 N-(4-phenylbutyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1A, substituting (4-isocyanatobutyl)benzene for methyl 4-isocyanatobenzoate and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for isoindoline. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.55 (s, 1H), 8.46 (d, J=5.0 Hz, 1H), 7.38 (d, J=5.1 Hz, 1H), 7.32-7.22 (m, 2H), 7.23-7.11 (m, 3H), 6.38 (t, J=5.6 Hz, 1H), 4.63-4.57 (m, 4H), 3.10-3.07 (m, 2H), 2.59 (t, J=7.5 Hz, 2H), 1.66-1.39 (m, 4H); MS (ESI(+)) m/e 296 (M+H)⁺.

Example 873 N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 873A N-benzyl-3-morpholino-N-(4-nitrophenethyl)propan-1-amine

A suspension of 1-(2-bromoethyl)-4-nitrobenzene (0.314 g, 1.366 mmol), N-benzyl-3-morpholinopropan-1-amine (0.128 g, 0.546 mmol), and potassium carbonate (0.189 g, 1.366 mmol) in dimethylformamide (1.821 ml) was heated at 65° C. for 20 hours. The reaction was partitioned in ethyl acetate and water. The organic layer was washed with brine, dried over anhydrous sodium sulfate, filtered, and concentrated. The concentrate was purified by flash chromatography to provide the title compound.

Example 873B 4-(2-(benzyl(3-morpholinopropyl)amino)ethyl)aniline

The title compound was prepared as described in Example 272A, substituting N-benzyl-3-morpholino-N-(4-nitrophenethyl)propan-1-amine for 4-nitro-N-propylbenzamide.

Example 873C N-[4-(2-{benzyl[3-(morpholin-4-yl)propyl]amino}ethyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-(2-(benzyl(3-morpholinopropyl)amino)ethyl)aniline for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.24 (s, 1H), 7.43 (d, J=8.5 Hz, 2H), 7.38-7.18 (m, 9H), 7.04 (d, J=8.5 Hz, 2H), 4.75 (s, 4H), 3.60 (s, 2H), 3.54-3.47 (m, 4H), 2.70-2.54 (m, 4H), 2.48-2.41 (m, 2H), 2.29-2.16 (m, 6H), 1.62-1.46 (m, 2H); MS (ESI(+)) m/e 499 (M+H)⁺.

Example 876 5-cyano-N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-amino-N-isopentylbenzenesulfonamide for 4-amino-N-propylbenzamide and isoindoline-5-carbonitrile for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.82 (s, 1H), 7.89 (s, 1H), 7.83-7.74 (m, 3H), 7.71-7.64 (m, 2H), 7.59 (d, J=7.9 Hz, 1H), 7.31 (t, J=5.8 Hz, 1H), 4.89-4.81 (m, 4H), 2.78-2.67 (m, 2H), 1.56 (dp, J=13.3, 6.7 Hz, 1H), 1.30-1.19 (m, 2H), 0.78 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 413 (M+H)⁺.

Example 877 N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-amino-N-isopentylbenzenesulfonamide for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.82 (s, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 7.81-7.74 (m, 2H), 7.71-7.64 (m, 2H), 7.44 (d, J=5.1 Hz, 1H), 7.32 (t, J=5.8 Hz, 1H), 4.87-4.80 (m, 4H), 2.78-2.67 (m, 2H), 1.56 (dp, J=13.3, 6.7 Hz, 1H), 1.30-1.13 (m, 2H), 0.78 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 389 (M+H)⁺.

Example 883 N-(4-{[(3-methoxybenzyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

N-(4-aminophenyl)isoindoline-2-carboxamide (0.0585 g, 0.231 mmol) was suspended in dichloromethane (2 ml) followed by addition of triisopropylethylamine (0.081 ml, 0.462 mmol). (3-Methoxyphenyl)methanesulfonyl chloride (0.061 g, 0.277 mmol) was dissolved in 1 ml dichloromethane and added to the mixture via syringe slowly. The mixture was quenched with water and the separated aqueous layer was extracted with dichloromethane. The combined organic layers were dried over magnesium sulfate, filtered and concentrated. Reverse-phase HPLC provided the title compound. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.65 (s, 1H), 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.34 (t, J=5.6 Hz, 1H), 7.80-7.73 (m, 2H), 7.69-7.61 (m, 2H), 7.44 (d, J=5.0 Hz, 1H), 4.86-4.79 (m, 4H), 3.20 (t, J=6.2 Hz, 2H), 2.46-2.25 (m, 3H), 2.20 (d, J=7.9 Hz, 3H), 2.06-1.78 (m, 1H), 1.52-1.37 (m, 1H); MS (ESI(+)) m/e 438 (M+H)⁺.

Example 909 N-{4-[6-(3-acetylphenyl)-4-(3-hydroxypropyl)-2-oxoquinolin-1(2H)-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 909A 6-bromo-4-(3-(tert-butyldiphenylsilyloxy)propyl)quinolin-2(1H)-one

6-Bromo-4-(3-hydroxypropyl)quinolin-2(1H)-one (4.7 g, 16.67 mmoles), imidazole (2.84 g, 41.7 mmoles) and tert-butyldiphenylsilyl chloride (5.14 mL, 20 mmoles) were stirred in dimethylformamide (60 mL) overnight at room temperature. The reaction mixture was poured into water and extracted with ethyl acetate twice. The organic layers were combined, dried over magnesium sulfate, filtered and concentrated. The crude product was purified by normal phase chromatography to provide the title compound.

Example 909B tert-butyl 4-(6-bromo-4-(3-(tert-butyldiphenylsilyloxy)propyl)-2-oxoquinolin-1(2H)-yl)butylcarbamate

The title compound was prepared as described in Example 797A, substituting 6-bromo-4-(3-(tert-butyldiphenylsilyloxy)propyl)quinolin-2(1H)-one for 6-bromoquinolin-2(1H)-one.

Example 909C 1-(4-aminobutyl)-6-bromo-4-(3-(tert-butyldiphenylsilyloxy)propyl)quinolin-2(1H)-one

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(6-bromo-4-(3-(tert-butyldiphenylsilyloxy)propyl)-2-oxoquinolin-1(2H)-yl)butylcarbamate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 909D N-(4-(6-bromo-4-(3-hydroxypropyl)-2-oxoquinolin-1(2H)-yl)butyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 1-(4-aminobutyl)-6-bromo-4-(3-(tert-butyldiphenylsilyloxy)propyl)quinolin-2(1H)-one for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride followed by TBAF deprotection and work up.

Example 909E N-{4-[6-(3-acetylphenyl)-4-(3-hydroxypropyl)-2-oxoquinolin-1(2H)-yl]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 280, substituting 3-acetylphenylboronic acid for 1H-pyrazol-3-ylboronic acid and N-(4-(6-bromo-4-(3-hydroxypropyl)-2-oxoquinolin-1(2H)-yl)butyl)isoindoline-2-carboxamide for 5-bromo-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, CDCl₃) δ ppm 8.24 (s, 1H), 8.08 (d, J=2.0 Hz, 1H), 7.96 (d, J=7.9 Hz, 1H), 7.87-7.79 (m, 2H), 7.58 (t, J=7.7 Hz, 1H), 7.54 (d, J=8.8 Hz, 1H), 7.28 (s, 4H), 6.71 (s, 1H), 4.74 (s, 4H), 4.41 (t, J=7.4 Hz, 2H), 3.82 (t, J=6.0 Hz, 2H), 3.46 (t, J=6.7 Hz, 2H), 3.12-2.99 (m, 2H), 2.68 (s, 3H), 2.10-1.96 (m, 2H), 1.96-1.83 (m, 2H), 1.79-1.72 (m, 2H); MS (APCI(+)) m/e 538 (M+H).

Example 910 N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 910A N-(4-(piperidin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide (2.0 g, 6.24 mmol) in 80 mL of 1:1 THF:methanol was added to 5% Pd on carbon (wet) (0.500 g) in a 250 mL SS pressure bottle and the mixture was stirred for 38 hours at 30 atm and 25° C. The mixture was filtered through a nylon membrane, concentrated and suspended in ether. Filtration with ether washes provided the title compound.

Example 910B N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(piperidin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and tetrahydrofuran-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.35 (s, 1H), 7.46 (m, 2H), 7.43 (d, J=5.0 Hz, 1H), 7.14 (m, 2H), 4.79 (m, 4H), 4.54 (m, 1H), 4.07 (m, 1H), 3.88 (dt, J=10.4, 8.1 Hz, 1H), 3.71 (m, 3H), 3.37 (m, 1H), 3.13 (m, 1H), 2.64-2.59 (m, 2H), 2.01 (m, 2H), 1.79 (m, 2H), 1.46 (m, 2H); MS (ESI(+)) m/e 421 (M+H).

TABLE 15 The following Examples were essentially prepared as described in Example 1C, substituting N- (4-(piperidin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan- 1-amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 911 N-(4-{1-[(2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.62 (m, 1H), (ESI(+)) methoxyethoxy)acetyl]pi- 8.51 (d, J = 7.4 Hz, 1H), 8.37 (s, 1H), 7.45 (m, 3H), m/e 439 peridin-4-yl}phenyl)-1,3- 7.13 (d, J = 8.6 Hz, 2H), 4.83 (m, 4H), 4.48 (m, 1H), (M + H)⁺ dihydro-2H-pyrrolo[3,4- 4.17 (m, 2H), 3.89 (m, 1H), 3.60 (m, 2H), 3.46 (m, c]pyridine-2- 2H), 3.26 (s, 3H), 3.07 (m, 1H), 2.78-2.56 (m, 2H), carboxamide 1.74 (m, 2H), 1.57 (m, 1H), 1.42 (m, 1H) 912 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) 2-ylcarbonyl)piperidin-4- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.48 (s, 2H), m/e 421 yl]phenyl}-1,3-dihydro- 7.43 (d, J = 5.0 Hz, 1H), 7.13 (m, 2H), 4.79 (m, 4H), (M + H)⁺ 2H-pyrrolo[3,4- 4.68 (dd, J = 7.6, 5.7 Hz, 1H), 4.49 (m, 1H), 4.11 (m, c]pyridine-2- 1H), 3.78 (m, 2H), 3.10 (m, 1H), 2.79-2.57 (m, carboxamide 2H), 2.03 (m, 2H), 1.84 (m, 4H), 1.61-1.36 (m, 2H) 913 N-{4-[1-(tetrahydro-2H- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) pyran-4- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.46 (m, 2H), m/e 435 ylcarbonyl)piperidin-4- 7.43 (d, J = 5.0 Hz, 1H), 7.13 (m, 2H), 4.79 (m, 4H), (M + H)⁺ yl]phenyl}-1,3-dihydro- 4.55 (m, 1H), 4.09 (m, 1H), 3.85 (m, 2H), 3.41 (m, 2H-pyrrolo[3,4- 2H), 3.10 (m, 1H), 2.91 (m, 1H), 2.71 (m, 1H), 2.58 c]pyridine-2- (m, 1H), 1.79 (m, 2H), 1.68-1.33 (m, 6H) carboxamide 914 N-{4-[1-(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) ylcarbonyl)piperidin-4- 8.50 (d, J = 4.9 Hz, 1H), 8.35 (s, 1H), 7.45 (m, 3H), m/e 437 yl]phenyl}-1,3-dihydro- 7.13 (s, 2H), 4.79 (d, J = 7.1 Hz, 4H), 4.45 (m, 1H), (M + H)⁺ 2H-pyrrolo[3,4- 4.34 (m, 1H), 4.07 (m, 1H), 3.80-3.55 (m, 5H), c]pyridine-2- 3.50 (m, 1H), 3.09 (m, 1H), 2.65 (m, 2H), 1.79 (m, carboxamide 2H), 1.67-1.29 (m, 2H) 915 N-(4-{1-[(1- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) methylpyrrolidin-3- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.47 (m, 2H), m/e 434 yl)carbonyl]piperidin-4- 7.43 (d, J = 5.0 Hz, 1H), 7.12 (m, 2H), 4.79 (m, 4H), (M + H)⁺ yl}phenyl)-1,3-dihydro- 4.49 (m, 1H), 4.16 (m, 1H), 3.58 (m, 4H), 3.26 (m, 2H-pyrrolo[3,4- 1H), 3.06 (m, 2H), 2.71 (m, 1H), 2.61 (m, 1H), 2.39 c]pyridine-2- (m, 4H), 1.78 (m, 2H), 1.57 (m, 1H), 1.40 (m, 1H) carboxamide 916 N-(4-{1-[(1,1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), (ESI(+)) dioxidotetrahydrothiophen- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.47 (m, 2H), m/e 469 3-yl)carbonyl]piperidin-4- 7.43 (d, J = 5.0 Hz, 1H), 7.14 (m, 2H), 4.79 (m, 4H), (M + H)⁺ yl}phenyl)-1,3-dihydro- 4.53 (m, 1H), 4.08 (m, 1H), 3.73 (m, 1H), 3.26- 2H-pyrrolo[3,4- 3.04 (m, 5H), 2.69 (m, 2H), 2.35 (m, 1H), 2.07 (m, c]pyridine-2- 1H), 1.81 (m, 2H), 1.51 (m, 2H) carboxamide 917 N-{4-[1-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) methylpropanoyl)piperidin- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.45 (m, 3H), m/e 409 4-yl]phenyl}-1,3- 7.13 (m, 2H), 5.38 (s, 1H), 4.75 (m, 4H), 4.60 (m, (M + H)⁺ dihydro-2H-pyrrolo[3,4- 2H), 2.95 (m, 1H), 2.80 (m, 2H), 1.77 (m, 2H), 1.48 c]pyridine-2- (m, 2H), 1.34 (s, 6H) carboxamide 918 N-{4-[1-(morpholin-4- ¹H NMR (500 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) ylacetyl)piperidin-4- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.47 (m, 2H), m/e 450 yl]phenyl}-1,3-dihydro- 7.43 (d, J = 5.0 Hz, 1H), 7.12 (m, 2H), 4.79 (m, 4H), (M + H)⁺ 2H-pyrrolo[3,4- 4.49 (m, 1H), 4.16 (m, 1H), 3.58 (m, 4H), 3.26 (m, c]pyridine-2- 1H), 3.06 (m, 2H), 2.71 (m, 1H), 2.61 (m, 1H), 2.39 carboxamide (m, 4H), 1.78 (m, 2H), 1.57 (m, 1H), 1.40 (m, 1H) 1279 N-(4-{1-[(2S)- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) tetrahydrofuran-2- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.46 (m, 2H), m/e 421 ylcarbonyl]piperidin-4- 7.43 (d, J = 5.1 Hz, 1H), 7.13 (m, 2H), 4.79 (m, 4H), (M + H)⁺ yl}phenyl)-1,3-dihydro- 4.68 (dd, J = 7.4, 5.8 Hz, 1H), 4.49 (d, J = 12.8 Hz, 2H-pyrrolo[3,4- 1H), 4.10 (m, 1H), 3.78 (m, 2H), 3.08 (m, 1H), 2.78- c]pyridine-2- 2.57 (m, 2H), 2.04 (m, 2H), 1.90-1.71 (m, 4H), carboxamide 1.61-1.32 (m, 2H) 1280 N-(4-{1-[(3S)- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) tetrahydrofuran-3- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.49-7.40 m/e 421 ylcarbonyl]piperidin-4- (m, 3H), 7.14 (m, 2H), 4.79 (m, 4H), 4.54 (m, 1H), (M + H)⁺ yl}phenyl)-1,3-dihydro- 4.06 (m, 1H), 3.88 (dt, J = 10.4, 8.1 Hz, 1H), 3.78- 2H-pyrrolo[3,4- 3.54 (m, 3H), 3.38 (m, 1H), 3.15 (m, 1H), 2.77- c]pyridine-2- 2.56 (m, 2H), 2.04 (m, 2H), 1.79 (m, 2H), 1.59- carboxamide 1.29 (m, 2H) 1384 N-(4-{1-[(2R)- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) tetrahydrofuran-2- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.45 (m, 3H), m/e 421 ylcarbonyl]piperidin-4- 7.13 (m, 2H), 4.79 (m, 4H), 4.68 (dd, J = 7.4, 5.8 Hz, (M + H)⁺ yl}phenyl)-1,3-dihydro- 1H), 4.48 (d, J = 12.7 Hz, 1H), 4.10 (d, J = 12.8 Hz, 2H-pyrrolo[3,4- 1H), 3.78 (m, 2H), 3.08 (dd, J = 26.0, 12.3 Hz, 1H), c]pyridine-2- 2.77-2.55 (m, 2H), 2.04 (m, 2H), 1.83 (m, 4H), carboxamide 1.62-1.32 (m, 2H) 1385 N-(4-{1-[(3R)- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), (ESI(+)) tetrahydrofuran-3- 8.50 (d, J = 5.0 Hz, 1H), 8.35 (s, 1H), 7.45 (m, 3H), m/e 421 ylcarbonyl]piperidin-4- 7.14 (m, 2H), 4.79 (m, 4H), 4.54 (m, 1H), 4.07 (m, (M + H)⁺ yl}phenyl)-1,3-dihydro- 1H), 3.88 (dt, J = 10.4, 8.1 Hz, 1H), 3.71 (m, 3H), 2H-pyrrolo[3,4- 3.37 (m, 1H), 3.10 (m, 1H), 2.80-2.55 (m, 2H), c]pyridine-2- 2.00 (m, 2H), 1.79 (m, 2H), 1.59-1.33 (m, 2H) carboxamide

Example 920 N-{5-[2-(2-chlorobenzyl)-1,3-thiazol-4-yl]-2-thienyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 920A 5-(2-(2-chlorobenzyl)thiazol-4-yl)thiophen-2-amine

The title compound was prepared as described in Example 806A, substituting 2-bromo-1-(5-nitrothiophen-2-yl)ethanone for 2-bromo-1-(4-nitrophenyl)ethanone and 2-(2-chlorophenyl)ethanethioamide for 2-phenylethanethioamide.

Example 920B N-{5-[2-(2-chlorobenzyl)-1,3-thiazol-4-yl]-2-thienyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 5-(2-(2-chlorobenzyl)thiazol-4-yl)thiophen-2-amine for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 9.73 (s, 1H), 7.46-7.55 (m, 3H), 7.34-7.40 (m, 4H), 7.28-7.34 (m, 2H), 7.20 (d, J=3.9 Hz, 1H), 6.62 (d, J=3.9 Hz, 1H), 4.76 (s, 4H), 4.45 (s, 2H); MS (ESI(+)) m/e 452.0 (M+H).

Example 921 N-[4-(4-fluorophenyl)butyl]-5-(hydroxymethyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-(4-fluorophenyl)butylamine for 4-amino-N-propylbenzamide and isoindolin-5-ylmethanol hydrochloride for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.28-7.17 (m, 5H), 7.13-7.03 (m, 2H), 6.29 (t, J=5.6 Hz, 1H), 5.16 (t, J=5.6 Hz, 1H), 4.54 (bs, 4H), 4.49 (d, J=5.5 Hz, 2H), 3.15-3.04 (m, 2H), 2.58 (t, J=7.4 Hz, 2H), 1.63-1.37 (m, 4H); MS (ESI(+)) m/e 343 (M+H)⁺.

Example 926 N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

In a 20 mL scintillation vial were mixed N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide (100 mg, 0.312 mmol), isobutyraldehyde (0.343 mmol), and sodium triacetoxyborohydride (0.43 mmol) in anhydrous dichloroethane (4 ml). The reaction mixture was stirred overnight at room temperature. This mixture was diluted with water and the resulting suspension was stirred again overnight at room temperature. The solid was filtered through a 30 mL plastic disposable Buchner funnel, and the collected solid was washed with water, dried for 2 hours, washed with ether, and dried again to provide the title compound. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.58 (s, 1H), 8.47 (d, J=5.0 Hz, 1H), 8.18 (m, 1H), 7.50 (m, 2H), 7.38 (d, J=5.1 Hz, 1H), 7.30 (m, 2H), 6.03 (m, 1H), 4.80 (m, 4H), 3.06 (m, 2H), 2.61 (t, J=5.6 Hz, 2H), 2.44 (m, 2H), 2.17 (d, J=7.2 Hz, 2H), 1.82 (m, 1H), 0.89 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 377 (M+H).

Example 927 N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 926, substituting tetrahydrofuran-3-carbaldehyde for isobutraldehyde. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.58 (s, 1H), 8.48 (d, J=5.0 Hz, 1H), 8.17 (bs, 1H), 7.60 (m, 2H), 7.38 (d, J=5.0 Hz, 1H), 7.30 (m, 2H), 6.05 (m, 1H), 4.83 (m, 4H), 3.77 (m, 2H), 3.62 (q, J=7.6 Hz, 1H), 3.39 (m, 1H), 3.10 (t, J=3.1 Hz, 2H), 2.95 (m, 1H), 2.65 (m, 2H), 2.43 (m, 2H), 2.38 (m, 2H), 1.95 (m, 1H), 1.54 (m, 1H); MS (ESI(+)) m/e 405 (M+H).

Example 928 N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 926, substituting tetrahydro-2H-pyran-4-carbaldehyde for isobutraldehyde. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ ppm 8.58 (s, 1H), 8.48 (d, J=5.0 Hz, 1H), 8.17 (bs, 1H), 7.50 (m, 2H), 7.38 (d, J=5.1 Hz, 1H), 7.30 (m, 2H), 6.03 (m, 1H), 4.79 (m, 4H), 3.83 (m, 2H), 3.31 (td, J=11.5, 2.2 Hz, 2H), 3.07 (m, 2H), 2.63 (t, J=5.6 Hz, 2H), 2.43 (m, 2H), 2.27 (d, J=7.1 Hz, 2H), 1.80 (m, 1H), 1.64 (m, 2H), 1.17 (m, 2H); MS (ESI(+)) m/e 419 (M+H).

Example 929 N-[4-(1-isobutylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 926, substituting N-(4-(piperidin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.33 (s, 1H), 7.43 (m, 3H), 7.13 (m, 2H), 4.79 (m, 4H), 2.41 (m, 1H), 2.92 (m, 2H), 2.15-1.85 (m, 4H), 1.85-1.50 (m, 5H), 0.87 (d, J=6.5 Hz, 6H); MS (ESI(+)) m/e 379 (M+H).

Example 930 N-{4-[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 926, substituting N-(4-(piperidin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide and tetrahydrofuran-3-carbaldehyde for isobutraldehyde. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.33 (s, 1H), 7.44 (m, 3H), 7.13 (m, 2H), 4.78 (m, 4H), 3.71 (m, 2H), 3.61 (q, J=7.6 Hz, 1H), 3.36 (m, 2H), 2.96 (m, 2H), 2.40 (m, 1H), 2.27 (m, 2H), 96 (m, 3H), 1.72 (m, 2H), 1.66-1.46 (m, 3H); MS (ESI(+)) m/e 407 (M+H).

Example 931 N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 926, substituting N-(4-(piperidin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide and tetrahydro-2H-pyran-4-carbaldehyde for isobutraldehyde. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.33 (s, 1H), 7.44 (m, 3H), 7.12 (m, 2H), 4.79 (m, 4H), 3.83 (m, 2H), 3.27 (m, 2H), 2.92 (m, 2H), 2.40 (m, 1H), 2.14 (d, J=7.2 Hz, 2H), 1.95 (m, 2H), 1.74 (m, 3H), 1.61 (m, 4H), 1.12 (m, 2H); MS (ESI(+)) m/e 421 (M+H).

Example 933 tert-butyl {4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]benzyl}carbamate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-aminobenzylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.29 (s, 1H), 7.52-7.45 (m, 2H), 7.40-7.24 (m, 5H), 7.15-7.08 (m, 2H), 4.76 (bs, 4H), 4.09-3.99 (m, 2H), 1.39 (s, 9H); MS (ESI(+)) m/e 368 (M+H)⁺.

Example 934 N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 934A N-(4-nitrophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 1A, substituting 1-isocyanato-4-nitrobenzene for methyl 4-isocyanatobenzoate and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for isoindoline.

Example 934B N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 272A, substituting N-(4-nitrophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 4-nitro-N-propylbenzamide.

Example 934C N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and cyclopentylacetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 9.70 (s, 1H), 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.34 (s, 1H), 7.51-7.40 (m, 5H), 4.82-4.75 (m, 4H), 2.33-2.17 (m, 3H), 1.81-1.68 (m, 2H), 1.68-1.43 (m, 4H), 1.27-1.13 (m, 2H); (ESI(+)) m/e 365 (M+H)⁺.

Example 936 N-[4-(5-{[(tetrahydrofuran-2-ylmethyl)amino]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 753B, substituting (tetrahydrofuran-2-yl)methanamine for morpholine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.68 (s, 1H), 7.91 (d, J=8.7 Hz, 2H), 7.79 (d, J=8.8 Hz, 2H), 7.45-7.20 (m, 4H), 4.80 (s, 4H), 4.08 (s, 2H), 3.95-3.78 (m, 1H), 3.79-3.66 (m, 1H), 3.66-3.49 (m, 1H), 2.66 (d, J=5.6 Hz, 2H), 2.00-1.67 (m, 4H), 1.67-1.41 (m, 2H), 1.40-1.16 (m, 2H), 0.87 (dd, J=9.3, 5.4 Hz, 1H); MS (ESI(+)) m/e 420 (M+H)⁺.

Example 937 N-(4-{5-[(4-methoxypiperidin-1-yl)methyl]-1,2,4-oxadiazol-3-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 753B, substituting 4-methoxypiperidine for morpholine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.69 (s, 1H), 7.92 (d, J=8.8 Hz, 2H), 7.80 (d, J=8.8 Hz, 2H), 7.45-7.20 (m, 4H), 4.80 (s, 4H), 3.93 (s, 2H), 3.21 (s, 3H), 3.20-3.10 (m, 1H), 2.82-2.68 (m, 2H), 2.50 (dt, J=3.6, 1.8 Hz, 2H), 2.41-2.24 (m, 2H), 1.92-1.75 (m, 2H), 1.56-1.37 (m, 2H); MS (ESI(+)) m/e 434 (M+H)⁺.

Example 938 N-[4-(5-{[4-(2-methoxyethyl)piperazin-1-yl]methyl}-1,2,4-oxadiazol-3-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 753B, substituting N-(2-methoxyethyl)piperazine for morpholine. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.69 (s, 1H), 7.92 (d, J=8.8 Hz, 2H), 7.86-7.70 (m, 2H), 7.46-7.23 (m, 4H), 4.80 (s, 4H), 3.93 (s, 2H), 3.40 (t, J=5.8 Hz, 3H), 3.21 (s, 3H), 2.55 (s, 4H), 2.45 (t, J=5.8 Hz, 6H); MS (ESI(+)) m/e 463 (M+H)⁺.

Example 940 N-{4-[(1-pentanoylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 940A tert-butyl 4-(4-nitrophenoxy)piperidine-1-carboxylate

4-Hydroxy-1-piperidine-1-carboxylic acid tert-butyl ester (6.04 g, 30 mmol) was dissolved in 1-fluoro-4-nitrobenzene (7.83 g, 55.5 mmol). Aqueous potassium hydroxide solution (25 percent wt, 44 mL) was added, followed by addition of tetrabutylammonium bromide (1.26 g). The reaction mixture was stirred at 35° C. for 17 hours. The solid was collected by filtration and washed with water (4×50 mL) to provide the title compound after vacuum drying.

Example 940B tert-butyl 4-(4-aminophenoxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 274, substituting tert-butyl 4-(4-nitrophenoxy)piperidine-1-carboxylate for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 940C tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenoxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(4-aminophenoxy)piperidine-1-carboxylate for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride.

Example 940D N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenoxy)piperidine-1-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 940E N-{4-[(1-pentanoylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and pentanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.80 (s, 1H), 8.68 (d, J=5.5 Hz, 1H), 8.36 (s, 1H), 7.77 (d, J=5.5 Hz, 1H), 7.42 (d, J=9.0 Hz, 1H), 6.95-6.87 (m, 2H), 4.87 (d, J=6.4 Hz, 4H), 4.64-4.45 (m, 1H), 3.92-3.79 (m, 1H), 3.76-3.63 (m, 1H), 3.38-3.15 (m, 2H), 2.31 (t, J=7.4 Hz, 2H), 1.96-1.81 (m, 2H), 1.61-1.41 (m, 4H), 1.38-1.22 (m, 2H), 0.88 (t, J=7.2 Hz, 3H); MS (ESI(+)) m/e 423 (M+H)⁺.

TABLE 16 The following Examples were essentially prepared as described in Example 940, substituting the appropriate alcohol, in place of 4-hydroxy-1-piperidine-1-carboxylic acid tert-butyl ester in Example 940A, and the appropriate carboxylic acid in Example 940E. Ex Name ¹H NMR MS 941 N-{4-[(1- 1H NMR (300 MHz, DMSO-d₆) δ 8.83 (s, 1H), 8.71 (ESI(+)) acetylpiperidin-4- (d, J = 5.6 Hz, 1H), 8.38 (s, 1H), 7.83 (d, J = 5.6 Hz, m/e 381 yl)oxy]phenyl}-1,3- 1H), 7.42 (d, J = 8.9 Hz, 2H), 6.91 (d, J = 9.0 Hz, (M + H)⁺ dihydro-2H- 2H), 4.89 (d, J = 9.8 Hz, 4H), 4.57-4.44 (m, 1H), pyrrolo[3,4- 3.91-3.76 (m, 1H), 3.76-3.57 (m, 1H), 3.43-3.12 c]pyridine-2- (m, 2H), 2.02 (s, 3H), 1.97-1.77 (m, 2H), 1.68-1.33 carboxamide (m, 2H) 942 N-{4-[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) butyrylpiperidin-4- (d, J = 5.0 Hz, 1H), 8.28 (s, 1H), 7.43 (dd, J = 7.0, 1.8 m/e 409 yl)oxy]phenyl}-1,3- Hz, 3H), 6.90 (d, J = 9.0 Hz, 2H), 4.78 (d, J = 4.0 Hz, (M + H)⁺ dihydro-2H- 4H), 4.57-4.39 (m, 1H), 3.95-3.76 (m, 1H), 3.70 pyrrolo[3,4- (d, J = 14.0 Hz, 1H), 3.23 (dd, J = 15.9, 6.4 Hz, 1H), c]pyridine-2- 2.30 (t, J = 7.4 Hz, 2H), 1.90 (s, 2H), 1.51 (dq, J = carboxamide 14.6, 7.3 Hz, 4H), 0.89 (t, J = 7.4 Hz, 3H) 943 N-(4-{[1-(2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.79 (s, 1H), 8.67 (ESI(+)) methylbutanoyl)pi- (d, J = 5.5 Hz, 1H), 8.36 (s, 1H), 7.76 (d, J = 5.5 Hz, m/e 423 peridin-4- 1H), 7.42 (d, J = 9.0 Hz, 1H), 6.91 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 1H), 4.87 (d, J = 5.8 Hz, 2H), 4.66-4.47 (m, 1H), dihydro-2H- 3.98-3.74 (m, 2H), 3.43-3.14 (m, 2H), 2.81-2.63 pyrrolo[3,4- (m, 1H), 1.99-1.82 (m, 2H), 1.55 (dt, J = 20.8, 7.2 c]pyridine-2- Hz, 1H), 1.31 (td, J = 13.9, 7.1 Hz, 1H), 0.98 (d, J = carboxamide 6.7 Hz, 3H), 0.81 (t, J = 7.4 Hz, 1H) 944 N-(4-{[1-(3,3,3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.80 (s, 1H), 8.68 (ESI(+)) trifluoropropanoyl)pi- (d, J = 5.5 Hz, 1H), 8.37 (s, 1H), 7.78 (d, J = 5.5 Hz, m/e 449 peridin-4- 1H), 7.42 (d, J = 8.9 Hz, 2H), 6.91 (d, J = 8.9 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.88 (d, J = 7.3 Hz, 5H), 4.60-4.44 (m, 1H), dihydro-2H- 3.85 (dd, J = 14.1, 5.4 Hz, 1H), 3.67 (q, J = 11.0 Hz, pyrrolo[3,4- 3H), 3.41-3.21 (m, 2H), 1.92 (dd, J = 16.5, 13.5 Hz, c]pyridine-2- 2H), 1.73-1.35 (m, 2H) carboxamide 945 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) (methoxyacetyl)pi- (d, J = 5.0 Hz, 1H), 8.28 (s, 1H), 7.43 (dd, J = 6.9, 1.9 m/e 411 peridin-4- Hz, 3H), 6.90 (d, J = 9.0 Hz, 2H), 4.78 (d, J = 3.9 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 5H), 4.51 (dd, J = 7.8, 3.9 Hz, 1H), 4.09 (s, 2H), 3.89- dihydro-2H- 3.74 (m, 1H), 3.62 (ddd, J = 8.2, 4.1, 1.1 Hz, 1H), pyrrolo[3,4- 3.29 (s, 3H), 1.91 (d, J = 1.3 Hz, 2H), 1.69-1.39 (m, c]pyridine-2- 2H) carboxamide 946 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.80 (s, 1H), 8.69 (ESI(+)) (tetrahydrofuran-2- (d, J = 5.5 Hz, 1H), 8.36 (s, 1H), 7.78 (d, J = 5.5 Hz, m/e 437 ylcarbonyl)piperidin- 1H), 7.42 (d, J = 9.0 Hz, 2H), 6.91 (d, J = 9.0 Hz, (M + H)⁺ 4-yl]oxy }phenyl)- 2H), 4.88 (d, J = 8.2 Hz, 4H), 4.76-4.62 (m, 1H), 1,3-dihydro-2H- 4.52 (s, 1H), 3.75 (dd, J = 12.0, 6.6 Hz, 5H), 3.48- pyrrolo[3,4- 3.14 (m, 2H), 1.91 (dddd, J = 19.4, 15.1, 7.6, 5.2 Hz, c]pyridine-2- 6H), 1.51 (dd, J = 20.6, 12.0 Hz, 2H) carboxamide 947 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) (cyclopropylcarbon- (d, J = 5.0 Hz, 1H), 8.27 (s, 1H), 7.43 (d, J = 8.9 Hz, m/e 407 yl)piperidin-4- 3H), 6.91 (d, J = 9.0 Hz, 2H), 4.78 (d, J = 4.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 4H), 4.53 (dt, J = 7.9, 4.0 Hz, 1H), 4.06-3.66 (m, dihydro-2H- 2H), 3.64-3.39 (m, 1H), 2.08-1.73 (m, 3H), 1.73- pyrrolo[3,4- 1.37 (m, 2H), 0.84-0.52 (m, 4H) c]pyridine-2- carboxamide 948 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) (cyclopropylacetyl) (d, J = 5.0 Hz, 1H), 8.27 (s, 1H), 7.42 (dd, J = 7.0, 1.8 m/e 421 piperidin-4- Hz, 2H), 6.90 (d, J = 9.0 Hz, 1H), 4.81-4.74 (m, (M + H)⁺ yl]oxy}phenyl)-1,3- 4H), 4.57-4.45 (m, 1H), 3.93-3.81 (m, 1H), 3.73- dihydro-2H- 3.62 (m, 1H), 2.27 (d, J = 6.7 Hz, 2H), 1.99-1.82 (m, pyrrolo[3,4- 2H), 1.68-1.35 (m, 2H), 1.04-0.87 (m, 1H), 0.50- c]pyridine-2- 0.40 (m, 2H), 0.16-0.07 (m, 2H) carboxamide 949 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.83 (s, 1H), 8.71 (ESI(+)) (cyclobutylcarbonyl) (d, J = 5.6 Hz, 1H), 8.37 (s, 1H), 7.82 (d, J = 5.6 Hz, m/e 421 piperidin-4- 1H), 7.41 (d, J = 9.0 Hz, 2H), 6.90 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.89 (d, J = 9.7 Hz, 4H), 4.61-4.38 (m, 1H), dihydro-2H- 3.90-3.75 (m, 1H), 3.64-3.46 (m, 1H), 3.27-3.06 pyrrolo[3,4- (m, 2H), 2.12 (ddd, J = 13.8, 12.3, 7.5 Hz, 4H), 2.00- c]pyridine-2- 1.77 (m, 3H), 1.74 (dd, J = 9.1, 4.8 Hz, 1H), 1.59- carboxamide 1.28 (m, 2H) 950 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.78 (s, 1H), 8.66 (ESI(+)) (cyclopentylcarbon- (d, J = 5.5 Hz, 1H), 8.35 (s, 1H), 7.74 (d, J = 5.4 Hz, m/e 435 yl)piperidin-4- 1H), 7.42 (d, J = 9.0 Hz, 2H), 6.91 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.87 (d, J = 4.5 Hz, 4H), 4.51 (dd, J = 7.7, 3.9 dihydro-2H- Hz, 1H), 3.92-3.70 (m, 2H), 3.45-3.30 (m, 1H), pyrrolo[3,4- 3.21 (dd, J = 18.3, 8.9 Hz, 1H), 2.98 (dd, J = 15.4, 7.5 c]pyridine-2- Hz, 1H), 2.01-1.38 (m, 12H) carboxamide 951 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.78 (s, 1H), 8.67 (ESI(+)) (cyclopentylacetyl)pi- (d, J = 5.4 Hz, 1H), 8.35 (s, 1H), 7.75 (d, J = 5.5 Hz, m/e 449 peridin-4- 1H), 7.42 (d, J = 9.0 Hz, 2H), 6.91 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.87 (d, J = 5.1 Hz, 5H), 4.55-4.45 (m, 1H), dihydro-2H- 3.86 (d, J = 12.3 Hz, 1H), 3.71 (d, J = 14.1 Hz, 1H), pyrrolo[3,4- 3.39-3.08 (m, 2H), 2.34 (d, J = 7.1 Hz, 2H), 2.13 (dt, c]pyridine-2- J = 15.3, 7.6 Hz, 1H), 1.90 (s, 2H), 1.74 (dt, J = 11.2, carboxamide 6.5 Hz, 2H), 1.65-1.36 (m, 6H), 1.23-1.02 (m, 2H) 952 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.78 (s, 1H), 8.66 (ESI(+)) (cyclohexylcarbon- (d, J = 5.4 Hz, 1H), 8.35 (s, 1H), 7.74 (d, J = 5.3 Hz, m/e 449 yl)piperidin-4- 1H), 7.42 (d, J = 9.0 Hz, 2H), 6.91 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.87 (d, J = 4.5 Hz, 4H), 4.54-4.44 (m, 1H), dihydro-2H- 3.83 (s, 2H), 3.17 (d, J = 0.9 Hz, 2H), 2.63-2.52 (m, pyrrolo[3,4- 1H), 1.91 (s, 3H), 1.61 (dd, J = 38.7, 30.1 Hz, 7H), c]pyridine-2- 1.43-1.02 (m, 7H) carboxamide 987 N-(4-{[1-(3,3,3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.77 (s, 1H), 8.65 (ESI(+)) trifluoropropanoyl)azetidin- (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.72 (d, J = 5.5 Hz, m/e 421 3-yl]oxy}phenyl)-1,3- 2H), 7.45 (d, J = 9.1 Hz, 2H), 6.78 (d, J = 9.1 Hz, (M + H)⁺ dihydro-2H- 2H), 5.06-4.93 (m, 1H), 4.87 (d, J = 3.6 Hz, 4H), pyrrolo[3,4- 4.60 (dd, J = 8.6, 6.5 Hz, 1H), 4.34 (dd, J = 11.0, 6.1 c]pyridine-2- Hz, 1H), 4.15 (dd, J = 9.6, 2.9 Hz, 1H), 3.81 (dd, J = carboxamide 10.7, 3.8 Hz, 1H), 3.40 (q, J = 11.2 Hz, 2H) 988 N-(4-{[1-(4,4,4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.69 (s, 1H), 8.58 (ESI(+)) trifluorobutanoyl)azetidin- (d, J = 5.3 Hz, 1H), 8.34 (s, 1H), 7.58 (d, J = 5.2 Hz, m/e 435 3-yl]oxy}phenyl)-1,3- 1H), 7.45 (d, J = 9.1 Hz, 2H), 6.78 (d, J = 9.0 Hz, (M + H)⁺ dihydro-2H- 2H), 4.98 (dd, J = 8.4, 4.4 Hz, 1H), 4.82 (s, 4H), 4.66- pyrrolo[3,4- 4.49 (m, 1H), 4.31 (dd, J = 10.6, 6.5 Hz, 1H), 4.13 c]pyridine-2- (dd, J = 9.4, 3.5 Hz, 1H), 3.78 (dd, J = 10.5, 3.7 Hz, carboxamide 2H), 2.40-2.29 (m, 4H) 989 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.57 (s, (ESI(+)) (tetrahydrofuran-2- 1H), 8.47 (d, J = 5.0 Hz, 1H), 8.06 (s, 1H), 7.50-7.39 m/e 409 ylcarbonyl)azetidin- (m, 2H), 7.37 (d, J = 4.9 Hz, 1H), 6.82-6.70 (m, 2H), (M + H)⁺ 3-yl]oxy}phenyl)- 4.98 (tt, J = 6.5, 4.1 Hz, 1H), 4.83-4.73 (m, 5H), 1,3-dihydro-2H- 4.34 (dd, J = 7.6, 6.2 Hz, 2H), 3.85-3.61 (m, 4H), pyrrolo[3,4- 2.10-1.90 (m, 2H), 1.90-1.70 (m, 2H) c]pyridine-2- carboxamide 990 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.57 (s, (ESI(+)) (tetrahydrofuran-3- 1H), 8.47 (d, J = 5.0 Hz, 1H), 8.06 (s, 1H), 7.50-7.41 m/e 423 ylacetyl)azetidin-3- (m, 2H), 7.37 (d, J = 5.0 Hz, 1H), 6.92-6.66 (m, 2H), (M + H)⁺ yl]oxy}phenyl)-1,3- 5.03-4.91 (m, 1H), 4.83-4.73 (m, 5H), 3.78 (dd, J = dihydro-2H- 8.3, 7.1 Hz, 1H), 3.71 (td, J = 8.1, 5.4 Hz, 1H), 3.62 pyrrolo[3,4- (dd, J = 15.4, 7.4 Hz, 1H), 3.27 (dd, J = 8.4, 6.5 Hz, c]pyridine-2- 1H), 2.24-2.09 (m, 3H), 2.05-1.89 (m, 1H), 1.50 carboxamide (dt, J = 14.7, 7.0 Hz, 1H) 991 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.64 (ESI(+)) (cyclobutylcarbonyl) (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.70 (d, J = 5.4 Hz, m/e 393 azetidin-3- 1H), 7.44 (d, J = 9.0 Hz, 2H), 6.77 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 5.05-4.90 (m, 1H), 4.86 (s, 4H), 4.52-4.40 (m, dihydro-2H- 1H), 4.30-4.20 (m, 1H), 3.97 (dd, J = 9.5, 3.8 Hz, pyrrolo[3,4- 1H), 3.74 (dd, J = 10.4, 3.8 Hz, 1H), 3.12 (p, J = 8.4 c]pyridine-2- Hz, 1H), 2.19-1.96 (m, 4H), 1.96-1.79 (m, 1H), carboxamide 1.79-1.62 (m, 1H) 992 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.77 (s, 1H), 8.66 (ESI(+)) (cyclopentylcarbon- (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.73 (d, J = 5.3 Hz, m/e 407 yl)azetidin-3- 1H), 7.45 (d, J = 9.0 Hz, 2H), 6.78 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.97 (t, J = 5.1 Hz, 1H), 4.87 (d, J = 3.9 Hz, 4H), dihydro-2H- 4.64-4.47 (m, 1H), 4.27 (dd, J = 10.3, 6.6 Hz, 1H), pyrrolo[3,4- 4.14-4.02 (m, 1H), 3.82-3.65 (m, 1H), 2.76-2.55 c]pyridine-2- (m, 1H), 1.89-1.39 (m, 8H) carboxamide 993 N-(4-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.80 (s, 1H), 8.68 (ESI(+)) phenylpropanoyl)pyrrolidin- (d, J = 5.4 Hz, 1H), 8.37 (s, 1H), 7.77 (d, J = 5.3 Hz, m/e 457 3-yl]oxy}phenyl)-1,3- 1H), 7.49-7.37 (m, 2H), 7.33-7.11 (m, 5H), 6.87 (M + H)⁺ dihydro-2H- (dd, J = 9.1, 2.3 Hz, 2H), 4.91 (dd, J = 22.6, 11.0 Hz, pyrrolo[3,4- 5H), 3.51 (d, J = 9.0 Hz, 4H), 2.81 (dd, J = 13.6, 7.3 c]pyridine-2- Hz, 2H), 2.63-2.51 (m, 2H), 2.07 (dd, J = 17.7, 8.2 carboxamide Hz, 2H) 994 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.49 (ESI(+)) (phenylacetyl)pyrrolidin-3- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.43 (dd, J = 6.8, 4.6 m/e 443 yl]oxy}phenyl)-1,3- Hz, 3H), 7.38-7.10 (m, 5H), 6.86 (dd, J = 8.9, 1.9 (M + H)⁺ dihydro-2H- Hz, 2H), 4.98 (d, J = 21.6 Hz, 1H), 4.78 (d, J = 4.4 pyrrolo[3,4- Hz, 4H), 3.59 (dd, J = 29.8, 8.4 Hz, 6H), 2.24-1.94 c]pyridine-2- (m, 2H) carboxamide 995 N-[4-({1-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.49 (ESI(+)) methoxyphenyl)ace- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.52-7.34 (m, 3H), m/e 473 tyl]pyrrolidin-3- 7.14 (t, J = 8.1 Hz, 2H), 6.95-6.73 (m, 4H), 4.97 (d, (M + H)⁺ yl}oxy)phenyl]-1,3- J = 21.7 Hz, 1H), 4.78 (d, J = 4.4 Hz, 4H), 3.70 (t, J = dihydro-2H- 10.2 Hz, 5H), 3.63-3.47 (m, 4H), 2.31-1.91 (m, pyrrolo[3,4- 2H) c]pyridine-2- carboxamide 996 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.82 (s, 1H), 8.70 (ESI(+)) (methoxyacetyl)pyr- (d, J = 5.5 Hz, 1H), 8.39 (s, 1H), 7.81 (d, J = 5.3 Hz, m/e 397 rolidin-3- 1H), 7.44 (d, J = 9.0 Hz, 2H), 6.96-6.81 (m, 2H), (M + H)⁺ yl]oxy}phenyl)-1,3- 4.91 (t, J = 9.8 Hz, 5H), 4.05 (s, 1H), 3.99 (s, 1H), dihydro-2H- 3.76-3.32 (m, 4H), 3.30 (s, 1.5H), 3.28 (s, 1.5H), pyrrolo[3,4- 2.13 (dd, J = 7.4, 3.7 Hz, 1H), 2.07-1.96 (m, 1H) c]pyridine-2- carboxamide 997 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) (cyclopropylcarbon- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.53-7.32 (m, 3H), m/e 393 yl)pyrrolidin-3- 6.89 (dd, J = 9.0, 7.4 Hz, 2H), 5.03 (dd, J = 18.0, 16.5 (M + H)⁺ yl]oxy}phenyl)-1,3- Hz, 1H), 4.78 (d, J = 3.8 Hz, 4H), 3.98-3.61 (m, dihydro-2H- 2H), 3.51 (m, 2H), 2.31-1.91 (m, 2H), 1.76 (d, J = pyrrolo[3,4- 20.7 Hz, 1H), 0.83-0.59 (m, 4H) c]pyridine-2- carboxamide 998 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.80 (s, 1H), 8.68 (ESI(+)) (cyclohexylcarbon- (d, J = 5.5 Hz, 1H), 8.37 (s, 1H), 7.77 (d, J = 5.0 Hz, m/e 435 yl)pyrrolidin-3- 1H), 7.43 (dd, J = 9.0, 1.8 Hz, 2H), 6.88 (dd, J = 9.0, (M + H)⁺ yl]oxy}phenyl)-1,3- 7.5 Hz, 2H), 5.01 (s, 1H), 4.89 (t, J = 8.6 Hz, 4H), dihydro-2H- 3.82-3.25 (m, 4H), 2.43-1.93 (m, 3H), 1.67 (d, J = pyrrolo[3,4- 10.0 Hz, 5H), 1.47-1.03 (m, 5H) c]pyridine-2- carboxamide 999 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.65 (ESI(+)) (cyclopentylace- (d, J = 5.4 Hz, 1H), 8.35 (s, 1H), 7.71 (d, J = 5.2 Hz, m/e 435 tyl)pyrrolidin-3- 1H), 7.44 (d, J = 8.6 Hz, 2H), 7.02-6.78 (m, 2H), (M + H)⁺ yl]oxy}phenyl)-1,3- 4.96 (d, J = 21.3 Hz, 1H), 4.86 (d, J = 2.2 Hz, 4H), dihydro-2H- 3.67-3.44 (m, 4H), 2.31-2.01 (m, 5H), 1.75 (s, 2H), pyrrolo[3,4- 1.62-1.38 (m, 4H), 1.10 (dd, J = 13.0, 5.9 Hz, 2H) c]pyridine-2- carboxamide 1000 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.64 (ESI(+)) (cyclopentylcarbon- (d, J = 5.4 Hz, 1H), 8.35 (s, 1H), 7.70 (d, J = 5.0 Hz, m/e 421 yl)pyrrolidin-3- 1H), 7.54-7.34 (m, 2H), 6.97-6.77 (m, 2H), 4.97 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 1H), 4.86 (s, 4H), 3.69-3.36 (m, 4H), 2.95-2.68 dihydro-2H- (m, 1H), 2.11 (ddd, J = 17.8, 8.5, 4.2 Hz, 2H), 1.86- pyrrolo[3,4- 1.41 (m, 8H) c]pyridine-2- carboxamide 1001 N-{4-[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.78 (d, J = 2.9 Hz, (ESI(+)) benzoylpyrrolidin-3- 1H), 8.67 (d, J = 4.0 Hz, 1H), 8.36 (d, J = 14.5 Hz, m/e 429 yl)oxy]phenyl}-1,3- 1H), 7.75 (d, J = 4.4 Hz, 1H), 7.61-7.33 (m, 7H), (M + H)⁺ dihydro-2H- 6.88 (dd, J = 27.8, 8.9 Hz, 2H), 4.98 (m, 1H), 4.87 (m, pyrrolo[3,4- 4H), 3.90-3.75 (m, 1H), 3.71-3.57 (m, 2H), 3.46 c]pyridine-2- (d, J = 24.5 Hz, 1H), 2.11 (d, J = 13.7 Hz, 2H) carboxamide 1002 N-(4-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.73 (s, 1H), 8.61 (ESI(+)) ethoxypropanoyl)pyr- (d, J = 5.3 Hz, 1H), 8.34 (s, 1H), 7.65 (d, J = 5.1 Hz, m/e 425 rolidin-3- 1H), 7.44 (dd, J = 9.0, 1.1 Hz, 2H), 6.88 (dd, J = 9.0, (M + H)⁺ yl]oxy}phenyl)-1,3- 5.3 Hz, 2H), 4.97 (d, J = 19.1 Hz, 1H), 4.84 (s, 4H), dihydro-2H- 3.62-3.47 (m, 6H), 3.47-3.32 (m, 4H), 2.19-2.09 pyrrolo[3,4- (m, 1H), 2.09-2.00 (m, 1H), 1.07 (dt, J = 9.8, 7.0 Hz, c]pyridine-2- 3H) carboxamide 1003 N-[4-({1-[(2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.78 (s, 1H), 8.66 (ESI(+)) methylcyclopropyl)car- (d, J = 5.4 Hz, 1H), 8.36 (s, 1H), 7.74 (d, J = 5.3 Hz, m/e 407 bonyl]pyrrolidin- 1H), 7.54-7.35 (m, 2H), 6.88 (td, J = 9.9, 5.3 Hz, (M + H)⁺ 3-yl}oxy)phenyl]- 2H), 4.99 (d, J = 30.6 Hz, 1H), 4.87 (d, J = 4.1 Hz, 1,3-dihydro-2H- 4H), 3.94-3.58 (m, 2H), 3.52 (t, J = 5.2 Hz, 2H), pyrrolo[3,4- 2.29-2.01 (m, 2H), 1.57-1.42 (m, 1H), 1.12-1.01 c]pyridine-2- (m, 4H), 0.94 (ddd, J = 9.5, 7.6, 4.7 Hz, 1H), 0.62- carboxamide 0.50 (m, 1H) 1004 N-[4-({1-[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.77 (s, 1H), 8.65 (ESI(+)) methylcyclopropyl)car- (d, J = 5.4 Hz, 1H), 8.36 (s, 1H), 7.72 (d, J = 5.4 Hz, m/e 407 bonyl]pyrrolidin- 1H), 7.57-7.37 (m, 2H), 6.88 (d, J = 9.0 Hz, 2H), (M + H)⁺ 3-yl}oxy)phenyl]- 4.97 (s, 1H), 4.87 (d, J = 3.5 Hz, 4H), 4.26 (s, 2H), 1,3-dihydro-2H- 3.77 (s, 2H), 2.10 (s, 2H), 1.26-1.17 (m, 3H), 0.92- pyrrolo[3,4- 0.80 (m, 1H), 0.66 (s, 1H), 0.48 (s, 2H) c]pyridine-2- carboxamide 1005 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.75 (s, 1H), 8.63 (ESI(+)) (cyclobutylcarbonyl) (d, J = 5.3 Hz, 1H), 8.34 (s, 1H), 7.68 (d, J = 5.1 Hz, m/e 407 pyrrolidin-3- 1H), 7.49-7.34 (m, 2H), 6.94-6.76 (m, 2H), 4.95 (M + H)⁺ yl]oxy}phenyl)-1,3- (d, J = 17.9 Hz, 1H), 4.85 (s, 4H), 3.67-3.10 (m, dihydro-2H- 5H), 2.10 (dtd, J = 19.7, 15.3, 8.2 Hz, 6H), 1.96-1.64 pyrrolo[3,4- (m, 2H) c]pyridine-2- carboxamide 1006 N-(4-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.79 (s, 1H), 8.67 (ESI(+)) methylbutanoyl)pyr- (d, J = 5.4 Hz, 1H), 8.37 (s, 1H), 7.75 (d, J = 5.4 Hz, m/e 409 rolidin-3- 1H), 7.44 (d, J = 9.0 Hz, 2H), 6.96-6.76 (m, 2H), (M + H)⁺ yl]oxy}phenyl)-1,3- 4.97 (d, J = 21.3 Hz, 1H), 4.87 (d, J = 5.4 Hz, 4H), dihydro-2H- 3.83-3.24 (m, 4H), 2.25-1.98 (m, 5H), 0.98-0.81 pyrrolo[3,4- (m, 6H) c]pyridine-2- carboxamide 1007 N-(4-{[1-(2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.65 (ESI(+)) methylpropanoyl)pyr- (d, J = 5.4 Hz, 1H), 8.36 (s, 1H), 7.71 (d, J = 5.0 Hz, m/e 395 rolidin-3- 1H), 7.44 (d, J = 8.8 Hz, 2H), 6.88 (dd, J = 9.0, 6.9 (M + H)⁺ yl]oxy}phenyl)-1,3- Hz, 2H), 4.97 (d, J = 25.9 Hz, 1H), 4.86 (d, J = 2.6 dihydro-2H- Hz, 4H), 3.80-3.26 (m, 4H), 2.64 (ddt, J = 21 A, pyrrolo[3,4- 13.9, 7.1 Hz, 1H), 2.31-2.00 (m, 2H), 0.99 (ddd, J = c]pyridine-2- 16.0, 9.0, 4.2 Hz, 6H) carboxamide 1008 N-{4-[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.79 (s, 1H), 8.67 (ESI(+)) acetylpyrrolidin-3- (d, J = 5.5 Hz, 1H), 8.37 (s, 1H), 7.75 (d, J = 5.4 Hz, m/e 367 yl)oxy]phenyl}-1,3- 1H), 7.44 (d, J = 8.9 Hz, 2H), 6.95-6.79 (m, 2H), (M + H)⁺ dihydro-2H- 5.07-4.90 (m, 1H), 4.87 (d, J = 5.3 Hz, 4H), 3.83- pyrrolo[3,4- 3.22 (m, 4H), 2.26-2.00 (m, 2H), 1.97 (s, 1.5H), 1.93 c]pyridine-2- (s, 1.5H) carboxamide 1009 N-(4-{[1-(4,4,4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.64 (ESI(+)) trifluorobutanoyl)pyr- (d, J = 5.4 Hz, 1H), 8.36 (s, 1H), 7.71 (d, J = 5.4 Hz, m/e 449 rolidin-3- 1H), 7.44 (dd, J = 9.0, 1.7 Hz, 2H), 6.88 (dd, J = 8.9, (M + H)⁺ yl]oxy}phenyl)-1,3- 6.4 Hz, 2H), 4.99 (d, J = 21.2 Hz, 1H), 4.86 (d, J = 2.1 dihydro-2H- Hz, 4H), 3.85-3.29 (m, 4H), 2.56 (d, J = 5.1 Hz, pyrrolo[3,4- 4H), 2.11 (dd, J = 24.1, 8.1 Hz, 2H) c]pyridine-2- carboxamide 1010 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.77 (s, 1H), 8.66 (ESI(+)) (tetrahydrofuran-3- (d, J = 5.4 Hz, 1H), 8.37 (s, 1H), 7.73 (d, J = 5.1 Hz, m/e 423 ylcarbonyl)pyrrolidin- 1H), 7.44 (dd, J = 8.9, 1.6 Hz, 2H), 6.89 (dd, J = 8.8, (M + H)⁺ 3-yl]oxy}phenyl)- 6.9 Hz, 2H), 4.98 (d, J = 21.7 Hz, 1H), 4.86 (d, J = 3.8 1,3-dihydro-2H- Hz, 4H), 3.95-3.46 (m, 8H), 3.20 (dd, J = 14.8, 7.8 pyrrolo[3,4- Hz, 1H), 1.97 (d, J = 7.5 Hz, 4H) c]pyridine-2- carboxamide 1011 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.80 (s, 1H), 8.68 (ESI(+)) (tetrahydrofuran-2- (d, J = 5.5 Hz, 1H), 8.38 (s, 1H), 7.78 (d, J = 5.4 Hz, m/e 423 ylcarbonyl)pyrrolidin- 1H), 7.44 (d, J = 9.0 Hz, 2H), 6.88 (dd, J = 8.2, 4.6 (M + H)⁺ 3-yl]oxy}phenyl)- Hz, 2H), 4.98 (d, J = 23.0 Hz, 1H), 4.88 (d, J = 7.4 1,3-dihydro-2H- Hz, 4H), 4.51 (dt, J = 13.2, 6.2 Hz, 2H), 3.89-3.46 pyrrolo[3,4- (m, 5H), 2.33-1.67 (m, 6H) c]pyridine-2- carboxamide 1012 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.79 (s, 1H), 8.67 (ESI(+)) (ethoxyacetyl)pyrrolidin- (d, J = 5.5 Hz, 1H), 8.38 (s, 1H), 7.76 (d, J = 5.1 Hz, m/e 411 3-yl]oxy}phenyl)-1,3- 1H), 7.44 (d, J = 9.0 Hz, 2H), 6.94-6.76 (m, 2H), (M + H)⁺ dihydro-2H- 4.98 (d, J = 22.7 Hz, 2H), 4.87 (d, J = 5.8 Hz, 5H), pyrrolo[3,4- 4.07 (s, 1H), 4.01 (s, 1H), 3.75-3.27 (m, 7H), 2.24- c]pyridine-2- 1.98 (m, 2H), 1.11 (dt, J = 10.8, 6.9 Hz, 3H) carboxamide 1026 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.77 (s, 1H), 8.65 (ESI(+)) (cyclohexylacetyl)pi- (d, J = 5.4 Hz, 1H), 8.34 (s, 1H), 7.72 (d, J = 5.4 Hz, m/e 463 peridin-4- 1H), 7.50-7.34 (m, 2H), 6.99-6.82 (m, 2H), 4.86 (M + H)⁺ yl]oxy}phenyl)-1,3- (d, J = 3.5 Hz, 4H), 4.56-4.45 (m, 1H), 3.60-3.89 (m, dihydro-2H- 2H), 3.39-3.14 (m, 2H), 2.20 (d, J = 6.7 Hz, 2H), pyrrolo[3,4- 1.90 (s, 2H), 1.72-1.39 (m, 8H), 1.29-1.06 (m, 3H), c]pyridine-2- 0.94 (t, J = 11.6 Hz, 2H) carboxamide 1027 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.79 (s, 1H), 8.67 (ESI(+)) (tetrahydro-2H- (d, J = 5.5 Hz, 1H), 8.36 (s, 1H), 7.76 (d, J = 5.5 Hz, m/e 465 pyran-4- 1H), 7.42 (d, J = 9.0 Hz, 2H), 6.91 (d, J = 9.0 Hz, (M + H)⁺ ylacetyl)piperidin-4- 2H), 4.87 (d, J = 6.1 Hz, 5H), 4.50 (dd, J = 7.7, 3.9 yl]oxy}phenyl)-1,3- Hz, 2H), 3.81 (ddd, J = 27.5, 21.4, 10.7 Hz, 4H), 3.39- dihydro-2H- 3.14 (m, 4H), 2.27 (d, J = 6.5 Hz, 2H), 2.01-1.77 pyrrolo[3,4- (m, 3H), 1.65-1.35 (m, 4H), 1.19 (tdd, J = 13.5, 9.2, c]pyridine-2- 4.4 Hz, 2H) carboxamide 1037 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.75 (s, 1H), 8.63 (ESI(+)) (tetrahydrofuran-2- (d, J = 5.4 Hz, 1H), 8.37 (s, 1H), 7.68 (d, J = 5.2 Hz, m/e 423 ylacetyl)azetidin-3- 1H), 7.45 (d, J = 9.0 Hz, 2H), 6.78 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.97 (dd, J = 10.3, 6.6 Hz, 1H), 4.85 (s, 4H), 4.63- dihydro-2H- 4.48 (m, 1H), 4.27 (s, 2H), 4.05 (dd, J = 13.5, 6.8 pyrrolo[3,4- Hz, 2H), 3.62-3.45 (m, 2H), 2.28 (dddd, J = 20.3, c]pyridine-2- 14.5, 10.4, 7.5 Hz, 3H), 2.06-1.90 (m, 1H), 1.81 (dd, carboxamide J = 13.8, 6.4 Hz, 2H), 1.47 (ddd, J = 15.7, 11.8, 7.2 Hz, 1H) 1038 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.77 (s, 1H), 8.65 (ESI(+)) (tetrahydro-2H- (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.71 (d, J = 5.5 Hz, m/e 437 pyran-4- 1H), 7.45 (d, J = 9.1 Hz, 2H), 6.78 (d, J = 9.0 Hz, (M + H)⁺ ylacetyl)azetidin-3- 2H), 4.96 (s, 1H), 4.86 (d, J = 3.0 Hz, 4H), 4.62-4.47 yl]oxy}phenyl)-1,3- (m, 1H), 4.27 (dd, J = 10.7, 6.3 Hz, 1H), 4.03 (dd, J = dihydro-2H- 14.3, 7.2 Hz, 1H), 3.76 (dd, J = 18.7, 8.0 Hz, 3H), pyrrolo[3,4- 3.25 (dd, J = 27.4, 15.8 Hz, 2H), 2.01 (t, J = 7.5 Hz, c]pyridine-2- 2H), 1.89 (s, 1H), 1.56 (d, J = 11.3 Hz, 2H), 1.34- carboxamide 1.03 (m, 2H) 1039 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.70 (s, 1H), 8.59 (ESI(+)) (morpholin-4- (d, J = 5.3 Hz, 1H), 8.37 (s, 1H), 7.59 (d, J = 5.1 Hz, m/e 438 ylacetyl)azetidin-3- 1H), 7.47 (d, J = 9.0 Hz, 2H), 6.80 (d, J = 9.0 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 5.06 (s, 1H), 4.83 (s, 4H), 4.65-4.53 (m, 1H), dihydro-2H- 4.44 (dd, J = 10.8, 6.2 Hz, 1H), 4.21-4.12 (m, 2H), pyrrolo[3,4- 4.07 (s, 5H), 3.23 (s, 4H) c]pyridine-2- carboxamide 1040 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.77 (s, 1H), 8.66 (ESI(+)) (cyclohexylacetyl)azetidin- (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.73 (d, J = 5.4 Hz, m/e 435 3-yl]oxy}phenyl)-1,3- 1H), 7.45 (d, J = 9.0 Hz, 2H), 6.78 (d, J = 9.0 Hz, (M + H)⁺ dihydro-2H-pyrrolo[3,4- 2H), 5.05-4.91 (m, 1H), 4.87 (d, J = 3.9 Hz, 4H), c]pyridine-2-carboxamide 4.62-4.45 (m, 1H), 4.27 (dd, J = 10.4, 6.5 Hz, 1H), 4.04 (dd, J = 9.1, 3.5 Hz, 1H), 3.74 (dd, J = 10.6, 3.7 Hz, 1H), 2.05-1.88 (m, 2H), 1.64 (d, J = 12.0 Hz, 6H), 1.16 (m, 3H), 0.94 (t, J = 11.8 Hz, 2H) 1041 N-(4-{[1-(2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.65 (ESI(+)) methylbutanoyl)azetidin- (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.71 (d, J = 5.4 Hz, m/e 395 3-yl]oxy}phenyl)-1,3- 1H), 7.51-7.37 (m, 2H), 6.79 (d, J = 9.0 Hz, 2H), (M + H)⁺ dihydro-2H-pyrrolo[3,4- 4.98 (d, J = 2.5 Hz, 1H), 4.86 (d, J = 2.9 Hz, 4H), 4.64- c]pyridine-2-carboxamide 4.48 (m, 1H), 4.33-4.21 (m, 1H), 4.12-4.02 (m, 1H), 3.76 (dd, J = 10.5, 3.8 Hz, 1H), 2.29 (dd, J = 13.8, 6.9 Hz, 1H), 1.58-1.39 (m, 1H), 1.39-1.20 (m, 1H), 0.97 (dd, J = 6.8, 4.1 Hz, 3H), 0.82 (q, J = 7.3 Hz, 3H) 1042 N-(4-{[1-(2, 2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.78 (s, 1H), 8.67 (ESI(+)) dimethylpropanoyl)azetidin- (d, J = 5.5 Hz, 1H), 8.39 (s, 1H), 7.74 (d, J = 5.4 Hz, m/e 395 3-yl]oxy}phenyl)-1,3- 1H), 7.54-7.33 (m, 2H), 6.82-6.64 (m, 2H), 4.94 (M + H)⁺ dihydro-2H-pyrrolo[3,4- (td, J = 6.3, 3.2 Hz, 1H), 4.87 (d, J = 4.8 Hz, 4H), 4.55- c]pyridine-2-carboxamide 4.12 (m, 4H), 1.12 (s, 9H) 1043 N-(4-{[1-(3, 3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.80 (s, 1H), 8.68 (ESI(+)) dimethylbutanoyl)azetidin- (d, J = 5.5 Hz, 1H), 8.39 (s, 1H), 7.77 (d, J = 5.5 Hz, m/e 409 3-yl]oxy}phenyl)-1,3- 1H), 7.44 (d, J = 9.0 Hz, 2H), 6.78 (d, J = 9.0 Hz, (M + H)⁺ dihydro-2H-pyrrolo[3,4- 2H), 5.01-4.90 (m, 1H), 4.88 (d, J = 6.5 Hz, 4H), c]pyridine-2-carboxamide 4.60-4.45 (m, 1H), 4.27 (dd, J = 10.4, 6.5 Hz, 1H), 4.04 (dd, J = 8.9, 5.2 Hz, 1H), 3.74 (dd, J = 10.6, 3.8 Hz, 1H), 1.96 (s, 2H), 0.98 (s, 9H) 1044 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.64 (ESI(+)) (tricyclo[3.3.1.1~3,7~]dec- (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.70 (d, J = 5.4 Hz, m/e 487 1-ylacetyl)azetidin-3- 1H), 7.52-7.36 (m, 2H), 6.82-6.69 (m, 2H), 4.97- (M + H)⁺ yl]oxy}phenyl)-1,3- 4.90 (m, 1H), 4.86 (s, 4H), 4.61-4.47 (m, 1H), 4.26 dihydro-2H- (dd, J = 10.3, 6.4 Hz, 1H), 4.08-3.99 (m, 1H), 3.74 pyrrolo[3,4- (dd, J = 10.6, 3.9 Hz, 1H), 1.92 (s, 2H), 1.83 (s, 2H), c]pyridine-2- 1.70-1.52 (m, 13H) carboxamide 1045 N-[4-({1-[(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.76 (s, 1H), 8.65 (ESI(+)) methoxycyclohexyl) (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.71 (d, J = 5.4 Hz, m/e 451 carbonyl]azetidin-3- 1H), 7.45 (d, J = 9.0 Hz, 2H), 6.78 (d, J = 9.0 Hz, (M + H)⁺ yl}oxy)phenyl]-1,3- 2H), 4.96 (s, 1H), 4.86 (d, J = 2.7 Hz, 4H), 4.58 (s, dihydro-2H- 1H), 4.31-4.19 (m, 1H), 4.05 (dd, J = 14.5, 7.4 Hz, pyrrolo[3,4- 1H), 3.74 (d, J = 10.3 Hz, 1H), 3.36 (s, 1H), 3.19 (s, c]pyridine-2- 3H), 2.27(s, 1H), 1.81 (s, 2H), 1.57 (t, J = 12.2 Hz, carboxamide 2H), 1.38 (s, 4H) 1288 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.57 (s, (ESI(+)) (tetrahydro-2H- 1H), 8.47 (d, J = 5.0 Hz, 1H), 8.06 (s, 1H), 7.50-7.40 m/e 423 pyran-2- (m, 2H), 7.37 (d, J = 5.0 Hz, 1H), 6.82-6.70 (m, 2H), (M + H)⁺ ylcarbonyl)azetidin- 4.97 (tt, J = 6.4, 4.0 Hz, 1H), 4.83-4.73 (m, 4H), 3-yl]oxy}phenyl)- 4.69-4.44 (m, 1H), 4.44-4.19 (m, 1H), 4.21-3.98 1,3-dihydro-2H- (m, 1H), 3.89 (ddd, J = 14.6, 10.3, 2.3 Hz, 3H), 3.48- pyrrolo[3,4- 3.33 (m, 1H), 1.79 (dt, J = 6.0, 4.3 Hz, 1H), 1.70 (dt, c]pyridine-2- J = 6.7, 2.5 Hz, 1H), 1.61-1.39 (m, 4H) carboxamide 1289 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.57 (s, (ESI(+)) (tetrahydro-2H- 1H), 8.47 (d, J = 5.0 Hz, 1H), 8.08-7.96 (m, 1H), m/e 437 pyran-2- 7.46-7.39 (m, 2H), 7.37 (d, J = 5.2 Hz, 1H), 6.84 (t, (M + H)⁺ ylcarbonyl)pyrrolidin- J = 5.9 Hz, 2H), 5.00-4.86 (m, 1H), 4.86-4.72 (m, 3-yl]oxy}phenyl)- 4H), 4.08-3.92 (m, 1H), 3.92-3.36 (m, 6H), 2.21- 1,3-dihydro-2H- 1.95 (m, 2H), 1.69-1.40 (m, 6H) pyrrolo[3,4- c]pyridine-2- carboxamide 1292 N-{4-[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.83 (s, 1H), 8.71 (ESI(+)) acetylpiperidin-3- (d, J = 5.4 Hz, 1H), 8.38 (s, 1H), 7.83 (dd, J = 5.2, 3.0 m/e 381 yl)oxy]phenyl}-1,3- Hz, 1H), 7.42 (dd, J = 8.9, 6.6 Hz, 2H), 6.89 (t, J = 8.5 (M + H)⁺ dihydro-2H- Hz, 2H), 4.89 (d, J = 9.6 Hz, 4H), 4.43 (s, 1H), 4.22- pyrrolo[3,4- 3.94 (m, 1H), 3.67-3.47 (m, 2H), 3.36-3.02 (m, c]pyridine-2- 1H), 2.02 (s, 1.5H), 1.87 (s, 1.5H), 1.83-1.32 (m, carboxamide 3H) 1293 N-{4-[(1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.66 (s, (ESI(+)) butanoylpiperidin-3- 1H), 8.55 (d, J = 5.3 Hz, 1H), 8.07 (s, 1H), 7.54 (d, m/e 409 yl)oxy]phenyl}-1,3- J = 5.1 Hz, 1H), 7.41 (d, J = 8.9 Hz, 2H), 6.95-6.70 (M + H)⁺ dihydro-2H- (m, 2H), 4.83 (s, 4H), 4.23 (bs, 2H), 3.45 (bs, 2H), pyrrolo[3,4- 2.24 (bs, 2H), 1.96 (bs, 1H), 1.73 (bs, 2H), 1.51 (dt, c]pyridine-2- J = 14.8, 7.4 Hz, 3H), 0.87 (t, J = 7.4 Hz, 3H) carboxamide 1294 N-(4-{[1-(3- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.65 (s, (ESI(+)) methylbutanoyl)pi- 1H), 8.54 (d, J = 5.2 Hz, 1H), 8.07 (s, 1H), 7.52 (d, m/e 423 peridin-3- J = 5.2 Hz, 1H), 7.41 (d, J = 8.9 Hz, 2H), 6.92-6.79 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 2H), 4.82 (s, 4H), 4.25 (bs, 2H), 3.46 (bs, 2H), dihydro-2H- 2.14 (s, 2H), 2.05-1.90 (m, 2H), 1.73 (bs, 2H), 1.45 pyrrolo[3,4- (bs, 1H), 0.90 (dd, J = 9.3, 6.5 Hz, 6H) c]pyridine-2- carboxamide 1295 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (ESI(+)) (methoxyacetyl)pi- (s, 1H), 8.54 (d, J = 5.2 Hz, 1H), 8.07 (s, 1H), 7.51 (d, m/e 411 peridin-3- J = 5.1 Hz, 1H), 7.42 (d, J = 9.0 Hz, 2H), 6.86 (d, J = (M + H)⁺ yl]oxy}phenyl)-1,3- 9.0 Hz, 2H), 4.82 (s, 4H), 4.26 (bs, 1H), 4.05 (d, J = dihydro-2H- 13.6 Hz, 1H), 3.96 (s, 1H), 3.42 (m, 4H), 3.27 (bs, pyrrolo[3,4- 3H), 1.93 (d, J = 28.0 Hz, 1H), 1.74 (bs, 2H), 1.49 (bs, c]pyridine-2- 1H) carboxamide 1296 N-(4-{[1-(2- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (ESI(+)) methylbutanoyl)pi- (s, 1H), 8.53 (d, J = 5.1 Hz, 1H), 8.06 (d, J = 2.1 Hz, m/e 423 peridin-3- 1H), 7.51 (d, J = 5.2 Hz, 1H), 7.44-7.38 (m, 2H), (M + H)⁺ yl]oxy}phenyl)-1,3- 6.85 (dd, J = 8.7, 1.2 Hz, 2H), 4.82 (s, 4H), 4.28- dihydro-2H- 4.17 (m, 1H), 3.67 (s, 2H), 3.51-3.37 (m, 2H), 2.65 pyrrolo[3,4- (s, 1H), 2.02-1.88 (m, 1H), 1.79-1.65 (m, 2H), 1.63- c]pyridine-2- 1.39 (m, 2H), 1.38-1.22 (m, 1H), 0.98 (dd, J = 6.7, carboxamide 4.4 Hz, 3H), 0.90-0.76 (m, 3H) 1297 N-(4-{[1-(3,3,3- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) trifluoropropanoyl)pi- 1H), 8.54 (d, J = 5.2 Hz, 1H), 8.08 (m, 1H), 7.52 (d, m/e 449 peridin-3- J = 5.1 Hz, 1H), 7.42 (d, J = 8.9 Hz, 2H), 6.86 (d, J = (M + H)⁺ yl]oxy}phenyl)-1,3- 9.0 Hz, 2H), 4.82 (m, 4H), 4.26 (s, 1H), 3.63-3.41 dihydro-2H- (m, 6H), 1.93 (d, J = 26.2 Hz, 1H), 1.75 (m, 2H), 1.49 pyrrolo[3,4- (m, 1H) c]pyridine-2- carboxamide 1298 N-(4-{[l- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (cyclopropylacetyl)pi- 1H), 8.53 (d, J = 5.2 Hz, 1H), 8.06 (s, 1H), 7.51 (d, m/e 421 peridin-3- J = 5.3 Hz, 1H), 7.48-7.35 (m, 2H), 6.92-6.79 (m, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.82 (s, 4H), 4.23 (m, 1H), 3.42-3.13 (m, 4H), dihydro-2H- 2.27 (d, J = 33.4 Hz, 3H), 1.93 (d, J = 26.2 Hz, 1H), pyrrolo[3,4- 1.72 (m, 2H), 1.46 (m, 1H), 0.95 (m, 1H), 0.43 (d, J = c]pyridine-2- 8.0 Hz, 2H), 0.09 (m, 2H) carboxamide 1299 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (cyclobutylcarbonyl) 1H), 8.53 (d, J = 5.1 Hz, 1H), 8.07 (bs, 1H), 7.50 (d, m/e 421 piperidin-3- J = 5.2 Hz, 1H), 7.45-7.39 (m, 2H), 6.88-6.82 (m, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.82 (s, 4H), 4.27-4.15 (m, 1H), 3.48-3.38 (m, dihydro-2H- 2H), 2.24-1.65 (m, 9H), 1.50-1.38 (m, 1H) pyrrolo[3,4- c]pyridine-2- carboxamide 1300 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (cyclobutylacetyl)pi- 1H), 8.53 (d, J = 5.1 Hz, 1H), 8.10-8.05 (m, 1H), m/e 435 peridin-3- 7.51 (d, J = 5.2 Hz, 1H), 7.42 (d, J = 7.7 Hz, 1H), 6.89- (M + H)⁺ yl]oxy}phenyl)-1,3- 6.82 (m, 2H), 4.82 (s, 4H), 4.51-3.84 (m, 1H), 2.67- dihydro-2H- 2.53 (m, 1H), 2.30 (d, J = 7.4 Hz, 1H), 2.11-1.91 pyrrolo[3,4- (m, 3H), 1.88-1.58 (m, 7H) c]pyridine-2- carboxamide 1301 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (cyclopentylcarbon- 1H), 8.53 (d, J = 5.2 Hz, 1H), 8.07 (s, 1H), 7.51 (d, m/e 435 yl)piperidin-3- J = 5.2 Hz, 1H), 7.42 (dd, J = 9.0, 3.7 Hz, 2H), 6.86 (d, (M + H)⁺ yl]oxy}phenyl)-1,3- J = 9.0 Hz, 2H), 4.82 (s, 4H), 4.45-3.57 (m, 5H), dihydro-2H- 2.92 (s, 2H), 1.97 (s, 1H), 1.67 (m, 12H) pyrrolo[3,4- c]pyridine-2- carboxamide 1302 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.65 (s, (ESI(+)) (cyclopentylacetyl)pi- 1H), 8.54 (d, J = 5.2 Hz, 1H), 8.07 (s, 1H), 7.52 (d, J = m/e 449 peridin-3- 5.2 Hz, 1H), 7.49-7.35 (m, 2H), 6.92-6.79 (m, (M + H)⁺ yl]oxy}phenyl)-1,3- 2H), 4.82 (s, 4H), 4.24 (s, 1H), 3.46 (s, 4H), 2.36- dihydro-2H- 2.07 (m, 3H), 1.93 (m, 1H), 1.73 (m, 4H), 1.51 (dd, J = pyrrolo[3,4- 22.2, 13.1 Hz, 5H), 1.13 (m, 2H) c]pyridine-2- carboxamide 1303 N-[4-({1-[(2S)- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (ESI(+)) tetrahy drofuran-2- (bs, 1H), 8.53 (m, 1H), 8.07 (bs, 1H), 7.51 (d, J = 5.2 m/e 437 ylcarbonyl]piperidin- Hz, 1H), 7.44-7.38 (m, 3H), 6.87 (dd, J = 9.0, 3.3 (M + H)⁺ 3-yl}oxy)phenyl]- Hz, 3H), 4.82 (s, 4H), 4.64-4.50 (m, 1H), 4.30-4.17 1,3-dihydro-2H- (m, 1H), 3.99-3.87 (m, 1H), 3.83-3.55 (m, 4H), pyrrolo[3,4- 2.03-1.68 (m, 7H), 1.48 (m, 1H) c]pyridine-2- carboxamide 1304 N-[4-({1-[(2R)- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (ESI(+)) tetrahydrofuran-2- (bs, 1H), 8.54 (m, 1H), 8.07 (bs, 1H), 7.52 (d, J = 4.8 m/e 437 ylcarbonyl]piperidin- Hz, 1H), 7.44-7.38 (m, 3H), 6.91-6.83 (m, 3H), (M + H)⁺ 3-yl}oxy)phenyl]- 4.82 (bs, 4H), 4.64-4.49 (m, 1H), 4.30-4.16 (m, 1,3-dihydro-2H- 1H), 3.93 (s, 1H), 3.43-3.20 (m, 3H), 2.05-1.75 (m, pyrrolo[3,4- 7H), 1.48 (s, 1H) c]pyridine-2- carboxamide 1305 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.62 (s, (ESI(+)) (tetrahydro-2H- 1H), 8.52 (d, J = 5.1 Hz, 1H), 8.06 (s, 1H), 7.53-7.42 m/e 451 pyran-4- (m, 2H), 7.41 (s, 1H), 6.91-6.79 (m, 2H), 4.81 (s, (M + H)⁺ ylcarbonyl)piperidin- 4H), 4.26 (s, 1H), 3.81 (m, 3H), 3.45 (s, 2H), 2.76 (s, 3-yl]oxy}phenyl)- 2H), 2.14 (m, 2H), 1.88-1.42 (m, 7H) 1,3-dihydro-2H- pyrrolo[3,4- c]pyridine-2- carboxamide 1306 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.62 (s, (ESI(+)) (tetrahydro-2H- 1H), 8.52 (d, J = 5.1 Hz, 1H), 8.06 (s, 1H), 7.47 (d, J = m/e 451 pyran-2- 5.2 Hz, 1H), 7.42 (dd, J = 9.1, 2.6 Hz, 2H), 6.86 (M + H)⁺ ylcarbonyl)piperidin- (dd, J = 9.0, 2.1 Hz, 2H), 4.81 (s, 4H), 4.08 (m, 3H), 3-yl]oxy}phenyl)- 3.93-3.54 (m, 3H), 3.28-3.13 (m, 2H), 2.00 (s, 1H), 1,3-dihydro-2H- 1.85-1.36 (m, 9H) pyrrolo[3,4- c]pyridine-2- carboxamide 1307 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (tetrahydro-2H- 1H), 8.54 (d, J = 5.2 Hz, 1H), 8.07 (s, 1H), 7.51 (d, J = m/e 465 pyran-4- 5.1 Hz, 1H), 7.42 (d, J = 8.9 Hz, 2H), 6.85 (d, J = (M + H)⁺ ylacetyl)piperidin-3- 9.0 Hz, 2H), 4.24 (s, 2H), 3.32 (dd, J = 50.2, 38.3 Hz, yl]oxy}phenyl)-1,3- 6H), 2.20 (m, 2H), 1.92 (m, 2H), 1.73 (m, 2H), 1.56 dihydro-2H- (m, 2H), 1.46 (m, 1H), 1.20 (m, 2H) pyrrolo[3,4- c]pyridine-2- carboxamide 1308 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.63 (s, (ESI(+)) (tetrahydrofuran-2- 1H), 8.52 (d, J = 5.2 Hz, 1H), 8.06 (s, 1H), 7.49 (d, m/e 451 ylacetyl)piperidin-3- J = 5.2 Hz, 1H), 7.42 (d, J = 8.8 Hz, 2H), 6.86 (d, J = (M + H)⁺ yl]oxy}phenyl)-1,3- 9.0 Hz, 2H), 4.81 (s, 5H), 4.37-4.03 (m, 2H), 3.71 (s, dihydro-2H- 2H), 3.63-3.50 (m, 3H), 2.61 (m, 2H), 2.44-2.25 pyrrolo[3,4- (m, 1H), 1.96 (m, 2H), 1.87-1.63 (m, 4H), 1.47 (m, c]pyridine-2- 2H) carboxamide 1309 N-(4-{[1- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.64 (s, (ESI(+)) (tetrahydrofuran-3- 1H), 8.54 (d, J = 5.2 Hz, 1H), 8.07 (s, 1H), 7.51 (d, J = m/e 451 ylacetyl)piperidin-3- 5.2 Hz, 1H), 7.42 (d, J = 8.9 Hz, 2H), 6.89-6.76 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 2H), 4.82 (s, 5H), 4.27 (s, 1H), 3.67-3.17 (m, dihydro-2H- 11H), 2.34 (d, J = 26.3 Hz, 3H), 1.93 (d, J = 29.4 Hz, pyrrolo[3,4- 3H), 1.73 (s, 3H), 1.47 (s, 3H) c]pyridine-2- carboxamide 1347 N-(4-{[1-(5-oxo-L- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) prolyl)piperidin-4- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.40 (d, m/e 450 yl]oxy}phenyl)-1,3- J = 8.54 Hz, 3H) 6.90 (d, J = 8.85 Hz, 2H) 4.79 (d, (M + H)⁺ dihydro-2H- J = 7.63 Hz, 4H) 4.45-4.58 (m, 2H) 3.75 (s, 2H) pyrrolo[3,4- 3.34-3.42 (m, 4H) 2.30-2.43 (m, 1H) 2.10-2.21 c]pyridine-2- (m, 2H) 1.94 (d, J = 5.80 Hz, 1H) 1.54-1.69 (m, 2H) carboxamide 1386 N-(4-{[1-(5-oxo-L- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) prolyl)azetidin-3- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.38-7.48 m/e 421 yl]oxy}phenyl)-1,3- (m, 3H) 6.75-6.83 (m, 2H) 4.98-5.06 (m, 1H) 4.79 (M + H)⁺ dihydro-2H- (d, J = 7.93 Hz, 4H) 4.29-4.72 (m, 2H) 4.18 (dd, pyrrolo[3,4- J = 8.39, 4.73 Hz, 1H) 3.64-4.12 (m, 2H) 2.06-2.41 c]pyridine-2- (m, 3H) 1.90-2.06 (m, 1H) carboxamide 1387 N-{4-[(1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) propanoylazetidin-3- ppm 8.57 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.38-7.46 m/e 367 yl)oxy]phenyl}-1,3- (m, 3H) 6.74-6.82 (m, 2H) 4.94-5.03 (m, 1H) 4.79 (M + H)⁺ dihydro-2H- (d, J = 7.02 Hz, 4H) 4.35 (s, 2H) 3.90 (s, 2H) 2.10 (q, pyrrolo[3,4- J = 7.43 Hz, 2H) 1.00 (t, J = 7.48 Hz, 3H) c]pyridine-2- carboxamide 1388 N-(4-{[1-(2, 2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) dimethylbutanoyl)azetidin- ppm 8.57 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.39-7.46 m/e 409 3-yl]oxy}phenyl)-1,3- (m, 3H) 6.78 (d, J = 8.85 Hz, 2H) 4.90-5.02 (m, 1H) (M + H)⁺ dihydro-2H-pyrrolo[3,4- 4.79 (d, J = 7.93 Hz, 4H) 4.51 (s, 2H) 4.01 (d, J = 8.54 c]pyridine-2-carboxamide Hz, 2H) 1.49 (q, J = 7.32 Hz, 2H) 1.09 (s, 6H) 0.81 (t, J = 7.48 Hz, 3H) 1389 N-(4-{[1-(2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) ethylbutanoyl)azetidin- ppm 8.57 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.37-7.47 m/e 409 3-yl]oxy}phenyl)- (m, 3H) 6.79 (d, J = 8.85 Hz, 2H) 4.95-5.03 (m, 1H) (M + H)⁺ 1,3-dihydro-2H- 4.79 (d, J = 7.93 Hz, 4H) 4.44 (s, 2H) 3.95 (s, 2H) pyrrolo[3,4- 2.08-2.22 (m, 1H) 1.32-1.55 (m, 4H) 0.83 (t, c]pyridine-2- J = 7.32 Hz, 6H) carboxamide 1390 N-(4-{[1-(pent-4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) ynoyl)azetidin-3- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.34-7.49 m/e 391 yl]oxy}phenyl)-1,3- (m, 3H) 6.78 (d, J = 8.85 Hz, 2H) 4.92-5.06 (m, 1H) (M + H)⁺ dihydro-2H- 4.79 (d, J = 7.93 Hz, 4H) 4.42 (d, J = 78.13 Hz, 2H) pyrrolo[3,4- 3.66-4.19 (m, 2H) 2.54 (t, J = 2.44 Hz, 1H) 2.27- c]pyridine-2- 2.43 (m, 4H) carboxamide 1391 N-(4-{[1-(furan-2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) ylcarbonyl)azetidin- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.77 (s, 1 m/e 405 3-yl]oxy}phenyl)- H) 7.37-7.48 (m, 3H) 7.04 (d, J = 3.66 Hz, 1H) 6.81 (M + H)⁺ 1,3-dihydro-2H- (d, J = 8.85 Hz, 2H) 6.57-6.63 (m, 1H) 5.01-5.14 pyrrolo[3,4- (m, 1H) 4.79 (d, J = 8.24 Hz, 4H) 4.67 (s, 2H) 4.17 c]pyridine-2- (s, 2H) carboxamide 1392 N-(4-{[1-(furan-3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) ylcarbonyl)azetidin- ppm 8.57 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 8.07 (s, 1 m/e 405 3-yl]oxy}phenyl)- H) 7.67 (s, 1H) 7.38-7.47 (m, 3H) 6.80 (d, J = 8.85 (M + H)⁺ 1,3-dihydro-2H- Hz, 2H) 6.72 (s, 1H) 5.03-5.11 (m, 1H) 4.79 (d, pyrrolo[3,4- J = 7.63 Hz, 4H) 4.60 (s, 2H) 4.12 (s, 2H) c]pyridine-2- carboxamide 1393 N-(4-{[1-(thiophen- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) 3- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.97 (d, m/e 421 ylcarbonyl)azetidin- J = 1.83 Hz, 1H) 7.55 (dd, J = 5.04, 2.90 Hz, 1H) 7.35- (M + H)⁺ 3-yl]oxy}phenyl)- 7.46 (m, 4H) 6.80 (d, J = 8.85 Hz, 2H) 5.01-5.11 (m, 1,3-dihydro-2H- 1H) 4.79 (d, J = 7.93 Hz, 4H) 4.62 (s, 2H) 4.16 (s, 2 pyrrolo[3,4- H) c]pyridine-2- carboxamide 1394 N-(4-{[1-(1H-pyrrol- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) 2- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.37-7.48 m/e 404 ylcarbonyl)azetidin- (m, 3H) 6.93 (s, 1H) 6.81 (d, J = 8.85 Hz, 2H) 6.51 (M + H)⁺ 3-yl]oxy}phenyl)- (d, J = 3.36 Hz, 1H) 6.14-6.18 (m, 1H) 5.02-5.14 1,3-dihydro-2H- (m, 1H) 4.79 (d, J = 7.93 Hz, 4H) 4.57-4.66 (m, 2H) pyrrolo[3,4- 4.13 (d, J = 7.93 Hz, 2H) c]pyridine-2- carboxamide 1395 N-(4-{[1-(pyrimidin- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) 4- ppm 9.09 (s, 1H) 8.75 (d, J = 2.14 Hz, 1H) 8.66 (s, 1 m/e 417 ylcarbonyl)azetidin- H) 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.37-7.47 (M + H)⁺ 3-yl]oxy}phenyl)- (m, 3H) 6.81 (d, J = 8.85 Hz, 2H) 5.06-5.13 (m, 1H) 1,3-dihydro-2H- 4.92-5.04 (m, 1H) 4.79 (d, J = 7.63 Hz, 4H) 4.50 (s, pyrrolo[3,4- 2 H) 4.09 (s, 1H) c]pyridine-2- carboxamide 1396 N-[4-({1-[(5- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) methylpyrazin-2- ppm 8.96 (s, 1H) 8.58 (s, 1H) 8.54 (s, 1H) 8.48 (d, m/e 431 yl)carbonyl]azetidin- J = 4.88 Hz, 1H) 7.38-7.47 (m, 3H) 6.80 (d, J = 8.85 (M + H)⁺ 3-yl}oxy)phenyl]- Hz, 2H) 5.04-5.13 (m, 1H) 4.89-5.02 (m, 1H) 1,3-dihydro-2H- 4.79 (d, J = 7.63 Hz, 4H) 4.48 (s, 2H) 4.06 (s, 1H) pyrrolo[3,4- 2.57 (s, 3H) c]pyridine-2- carboxamide 1397 N-(4-{[1-(N,N- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (APCI(+)) dimethylglycyl)azetidin- Temp = 90° C.) δ ppm 8.57-8.59 (bs, 1H), 8.48 (dd, J = m/e 396 3-yl]oxy}phenyl)-1,3- 4.9, 1.8 Hz, 1H), 7.43-7.47 (m, 2H), 7.41 (d, J = 6.7 (M + H)⁺ dihydro-2H- Hz, 1H), 6.80-6.83 (m, 2H), 5.08-5.16 (m, 1H), 4.82 pyrrolo[3,4- (s, 2H), 4.79 (s, 2H), 4.67-4.74 (m, 2H), 4.30 (dd, J = c]pyridine-2- 10.1, 4.1 Hz, 2H), 2.91 (s, 8H) carboxamide 1398 N-(4-{[1-(N, N- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (APCI(+)) dimethyl-beta- Temp = 90° C.) δ ppm 8.57 (s, 1H), 8.48 (d, J = 5.2 Hz, m/e 410 alanyl)azetidin-3- 1H), 7.44-7.48 (m, 2H), 7.40 (d, J = 4.6 Hz, 1H), (M + H)⁺ yl]oxy}phenyl)-1,3- 6.80-6.84 (m, 2H), 5.09-5.16 (m, 1H), 4.83 (s, 2H), dihydro-2H- 4.79 (s, 2H), 4.70 (ddd, J = 10.4, 6.6, 1.2 Hz, 2H), pyrrolo[3,4- 4.30 (ddd, J = 10.4, 4.1, 1.2 Hz, 2H), 2.91 (s, 6H), c]pyridine-2- 2.50 (t, J = 7.3 Hz, 2H), 2.23 (t, J = 7.2 Hz, 2H) carboxamide 1399 N-(4-{[1-(pyrrolidin- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (APCI(+)) 1-ylacetyl)azetidin- Temp = 90° C.) δ ppm 8.58 (s, 1H), 8.48 (dd, J = 5.2, 1.8 m/e 422 3-yl]oxy}phenyl)- Hz, 1H), 7.43-7.47 (m, 2H), 7.40 (d, J = 5.2 Hz, 1H), (M + H)⁺ 1,3-dihydro-2H- 6.80-6.84 (m, 2H), 5.09-5.16 (m, 1H), 4.82 (s, 2H), pyrrolo[3,4- 4.79 (s, 2H), 4.70 (ddd, J = 10.2, 6.4, 1.1 Hz, 2H), c]pyridine-2- 4.30 (ddd, J = 10.3, 4.2, 1.1 Hz, 2H), 3.18 (s, 2H), carboxamide 2.55-2.62 (m, 4H), 1.68-1.75 (m, 4H) 1400 N-[4-({-[3- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (APCI(+)) (pyrrolidin-1- Temp = 90° C.) δ ppm 8.57-8.58 (bs, 1H), 8.48 (dd, J = m/e 436 yl)propanoyl]azetidin- 5.0, 2.0 Hz, 1H), 7.41-7.45 (m, 2H), 7.40 (d, J = 4.9 (M + H)⁺ 3-yl}oxy)phenyl]- Hz, 1H), 6.76-6.80 (m, 2H), 4.94-5.01 (m, 1H), 4.82 1,3-dihydro-2H- (s, 2H), 4.79 (s, 2H), 4.19-4.64 (m, 2H), 3.70-4.17 (m, pyrrolo[3,4- 2H), 2.66 (t, J = 7.3 Hz, 2H), 2.44-2.50 (m, 4H), 2.27 c]pyridine-2- (t, J = 7.3 Hz, 2H), 1.65-1.71 (m, 4H) carboxamide 1401 N-[4-({1-[3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) (piperidin-1- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.35-7.48 m/e 450 yl)propanoyl]azetidin- (m, 3H) 6.74-6.83 (m, 2H) 4.92-5.02 (m, 1H) 4.79 (M + H)⁺ 3-yl}oxy)phenyl]- (d, J = 7.93 Hz, 4H) 4.18-4.71 (m, 2H) 3.94 (d, 1,3-dihydro-2H- J = 92.77 Hz, 2H) 2.53-2.58 (m, 2H) 2.32-2.40 (m, pyrrolo[3,4- 4H) 2.24 (t, J = 7. 17 Hz, 2H) 1.44-1.54 (m, 4H) 1.33- c]pyridine-2- 1.41 (m, 2H) carboxamide 1402 N-[4-({1-[(4- ¹H NMR (400 MHz, DMSO-d₆/Deuterium Oxide, (APCI(+)) methylpiperazin-1- Temp = 90° C.) δ ppm 8.58 (s, 1H), 8.48 (dd, J = 5.0, m/e 451 yl)acetyl]azetidin-3- 2.0 Hz, 1H), 7.41-7.45 (m, 2H), 7.40 (d, J = 5.2 Hz, 1H), (M + H)⁺ yl}oxy)phenyl]-1,3- 6.75-6.80 (m, 2H), 5.08-5.17 (m, 1H), 4.82 (s, 2H), dihydro-2H- 4.79 (s, 2H), 4.70 (ddd, J = 10.0, 6.3, 1.3 Hz, 2H), pyrrolo[3,4- 4.30 (ddd, J = 10.0, 4.0, 1.0 Hz, 2H), 3.00 (s, 2H), c]pyridine-2- 2.41-2.48 (m, 4H), 2.30-2.37 (m, 4H), 2.15 (s, 3H) carboxamide 1403 N-[4-({1-[3-(4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) methylpiperazin-1- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.38-7.48 m/e 456 yl)propanoyl]azetidin- (m, 3H) 6.78 (d, J = 9.16 Hz, 2H) 4.93-5.01 (m, 1H) (M + H)⁺ 3-yl}oxy)phenyl]- 4.79 (d, J = 7.93 Hz, 4H) 4.19-4.64 (m, 2H) 3.94 (d, 1,3-dihydro-2H- J = 87.28 Hz, 2H) 2.53-2.58 (m, 2H) 2.36-2.43 (m, pyrrolo[3,4- 4H) 2.29-2.35 (m, 4H) 2.24 (t, J = 7.17 Hz, 2H) 2.15 c]pyridine-2- (s, 3H) carboxamide 1423 N-[4-({1-[(2S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) methylbutanoyl]pi- (d, J = 5.0 Hz, 1H), 8.27 (s, 1H), 7.51-7.34 (m, 3H), m/e 423 peridin-4- 6.90 (d, J = 9.0 Hz, 2H), 4.78 (d, J = 4.0 Hz, 4H), (M + H)⁺ yl}oxy)phenyl]-1,3- 4.60-4.44 (m, 1H), 3.84 (d, J = 39.0 Hz, 2H), 3.46-3.12 dihydro-2H- (m, 2H), 2.73 (dd, J = 13.4, 6.8 Hz, 1H), 1.99 (s, 2H), pyrrolo[3,4- 1.55 (dt, J = 21.7, 7.3 Hz, 3H), 1.42-1.21 (m, 1H), c]pyridine-2- 0.97 (t, J = 5.7 Hz, 3H), 0.81 (t, J = 7.4 Hz, 3H) carboxamide 1424 N-[4-({1-[(2S)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) tetrahydrofuran-2- (d, J = 5.0 Hz, 1H), 8.28 (s, 1H), 7.46-7.39 (m, 3H), m/e 437 ylcarbonyl]piperidin- 6.94-6.87 (m, 2H), 4.86-4.74 (m, 4H), 4.67 (t, J = (M + H)⁺ 4-yl}oxy)phenyl]- 6.6 Hz, 1H), 4.57-4.46 (m, 1H), 3.93-3.67 (m, 4H), 1,3-dihydro-2H- 3.31 (s, 2H), 2.12-1.77 (m, 6H), 1.65-1.39 (m, 2H) pyrrolo[3,4- c]pyridine-2- carboxamide 1425 N-[4-({1-[(2R)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) tetrahy drofuran-2- (d, J = 5.0 Hz, 1H), 8.27 (s, 1H), 7.53-7.33 (m, 3H), m/e 437 ylcarbonyl]piperidin- 6.90 (d, J = 9.0 Hz, 2H), 4.78 (d, J = 4.0 Hz, 4H), 4.73- (M + H)⁺ 4-yl}oxy)phenyl]- 4.60 (m, 1H), 4.52 (s, 1H), 3.93-3.63 (m, 4H), 3.49- 1,3-dihydro-2H- 3.07 (m, 2H), 2.11-1.72 (m, 6H), 1.66-1.40 (m, pyrrolo[3,4- 2H) c]pyridine-2- carboxamide 1426 N-[4-({1-[(4,4- ¹H NMR (400 MHz, DMSO, Temp = 90° C.) δ 8.57 (s, (ESI(+)) difluorocyclohexyl)carbon- 1H), 8.47 (d, J = 5.0 Hz, 1H), 8.05 (d, J = 8.0 Hz, m/e 457 yl]azetidin-3- 1H), 7.48-7.39 (m, 2H), 7.37 (d, J = 4.8 Hz, 1H), (M + H)⁺ yl}oxy)phenyl]-1,3- 6.86-6.60 (m, 2H), 4.96 (m, 1H), 4.78 (d, J = 8.8 Hz, dihydro-2H- 5H), 4.19 (m, 2H), 3.74 (m, 2H), 3.22 (d, J = 6.2 Hz, pyrrolo[3,4- 1H), 2.42 (t, J = 10.6 Hz, 1H), 2.26 (t, J = 6.9 Hz, c]pyridine-2- 1H), 2.04 (d, J = 10.0 Hz, 2H), 1.81 (ddd, J = 26.3, carboxamide 15.5, 8.4 Hz, 3H), 1.68-1.49 (m, 2H) 1427 N-(4-{[1-(5-oxo-D- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) prolyl)piperidin-4- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.40 (d, m/e 450 yl]oxy}phenyl)-1,3- J = 8.54 Hz, 3H) 6.90 (d, J = 8.85 Hz, 2H) 4.79 (d, (M + H)⁺ dihydro-2H- J = 7.63 Hz, 4H) 4.46-4.60 (m, 2H) 3.75 (s, 2H) pyrrolo[3,4- 3.34-3.41 (m, 2H) 2.30-2.41 (m, 1H) 2.10-2.23 c]pyridine-2- (m, 2H) 1.92-2.05 (m, 3H) 1.56-1.74 (m, 2H) carboxamide 1428 N-(4-{[1-(2,2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) dimethylpropanoyl)pi- ppm 8.58 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.36-7.44 m/e 423 peridin-4- (m, 3H) 6.89 (d, J = 8.85 Hz, 2H) 4.79 (d, J = 7.32 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 4H) 4.43-4.53 (m, 1H) 3.80-3.93 (m, 2H) 3.34- dihydro-2H- 3.42 (m, 2H) 1.94-1.99 (m, J = 3.36 Hz, 2H) 1.50- pyrrolo[3,4- 1.68 (m, 2H) 1.22 (s, 9H) c]pyridine-2- carboxamide 1429 N-(4-{[1-(2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) methylpentanoyl)pi- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.40 (d, m/e 437 peridin-4- J = 8.85 Hz, 3H) 6.89 (d, J = 8.85 Hz, 2H) 4.79 (d, (M + H)⁺ yl]oxy}phenyl)-1,3- J = 7.32 Hz, 4H) 4.45-4.54 (m, 1H) 3.81 (dd, dihydro-2H- J = 11.14, 5.34 Hz, 2H) 3.35 (s, H) 2.75-2.84 (m, 1 pyrrolo[3,4- H) 1.93-1.98 (m, 2H) 1.49-1.64 (m, 3H) 1.19- c]pyridine-2- 1.35 (m, 3H) 1.01 (d, J = 6.71 Hz, 3H) 0.86 (t, J = 7.02 carboxamide Hz, 3H) 1430 N-(4-{[1-(2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) ethylbutanoyl)pi- ppm 8.58 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.40 (d, m/e 437 peridin-4- J = 9.16 Hz, 3H) 6.90 (d, J = 8.85 Hz, 2H) 4.79 (d, (M + H)⁺ yl]oxy}phenyl)-1,3- J = 7.63 Hz, 4H) 4.46-4.56 (m, J = 11.22, 7.40, 3.66 dihydro-2H- Hz, 1H) 3.80-3.92 (m, 2H) 3.35-3.43 (m, 2H) pyrrolo[3,4- 2.58-2.68 (m, 1H) 1.87-1.95 (m, 2H) 1.47-1.64 c]pyridine-2- (m, 4H) 1.34-1.46 (m, 2H) 0.82 (t, J = 7.48 Hz, 6H) carboxamide 1431 N-(4-{[1-(1H-pyrrol- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) 2- ppm 8.57 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.37-7.46 m/e 432 ylcarbonyl)piperidin- (m, 3H) 6.85-6.95 (m, 3H) 6.49 (d, J = 3.05 Hz, 1H) (M + H)⁺ 4-yl]oxy}phenyl)- 6.13 (t, J = 2.90 Hz, 1H) 4.79 (d, J = 7.93 Hz, 4H) 4.47- 1,3-dihydro-2H- 4.60 (m, 1H) 3.93-4.09 (m, 2H) 3.49-3.59 (m, 2 pyrrolo[3,4- H) 1.95-2.03 (m, 2H) 1.56-1.74 (m, 2H) c]pyridine-2- carboxamide 1432 N-(4-{[1-(1,2- ¹H NMR (400 MHz, Solvent) δ ppm 8.57 (s, 1H) 8.47 (APCI(+)) oxazol-5- (d, J = 4.88 Hz, 1H) 7.36-7.44 (m, 3H) 6.89 (d, m/e 434 ylcarbonyl)piperidin- J = 8.54 Hz, 2H) 4.79 (d, J = 7.93 Hz, 4H) 3.44-4.62 (M + H)⁺ 4-yl]oxy}phenyl)- (m, 4H) 1.79-1.89 (m, 2H) 1.40-1.80 (m, 3H) 1,3-dihydro-2H- pyrrolo[3,4- c]pyridine-2- carboxamide 1433 N-(4-{[1-(pyridin-3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) ylcarbonyl)piperidin- ppm 8.62 (d, J = 4.58 Hz, 1H) 8.58 (d, J = 7.32 Hz, 2H) m/e 444 4-yl]oxy}phenyl)- 8.47 (d, J = 5.19 Hz, 1H) 7.82 (d, J = 7.93 Hz, 1H) 7.47 (M + H)⁺ 1,3-dihydro-2H- (dd, J = 7.63,4.88 Hz, 1H) 7.40 (d, J = 8.54 Hz, 3H) pyrrolo[3,4- 6.91 (d, J = 8.85 Hz, 2H) 4.79 (d, J = 7.63 Hz, 4H) 4.50- c]pyridine-2- 4.58 (m, 1H) 3.75 (s, 2H) 3.38-3.50 (m, J = 8.85 carboxamide Hz, 2H) 1.93-2.05 (m, 2H) 1.62-1.76 (m, 2H) 1434 N-(4-{[1-(pyridazin- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) 3-ylcarbonyl)piperidin- ppm 9.26 (dd, J = 4.58, 2.14 Hz, 1H) 8.58 (s, 1H) 8.49 m/e 445 4-yl]oxy}phenyl)- (d, J = 4.88 Hz, 1H) 7.76-7.85 (m, 2H) 7.37-7.45 (M + H)⁺ 1,3-dihydro-2H- (m, 3H) 6.91 (t, J = 9.16 Hz, 2H) 4.80 (d, J = 6.10 Hz, pyrrolo[3,4- 4H) 4.48-4.63 (m, 1H) 3.99 (s, 2H) 3.60 (s, 2H) c]pyridine-2- 1.95-2.14 (m, 2H) 1.72 (s, 2H) carboxamide 1435 N-(4-{[1-(pyrazin-2- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) ylcarbonyl)piperidin- ppm 9.20 (s, 1H) 8.93 (d, J = 5.19 Hz, 1H) 8.57 (s, 1 m/e 445 4-yl]oxy}phenyl)- H) 8.47 (d, J = 4.88 Hz, 1H) 7.60-7.65 (m, 1H) 7.36- (M + H)⁺ 1,3-dihydro-2H- 7.44 (m, 3H) 6.87-6.94 (m, 2H) 4.79 (d, J = 7.63 pyrrolo[3,4- Hz, 4H) 4.47-4.62 (m, 1H) 3.94 (s, 2H) 3.55 (s, 2 c]pyridine-2- H) 1.93-2.11 (m, 2H) 1.61-1.78 (m, J = 15.87 Hz, 2 carboxamide H) 1436 N-(4-{[1-(pyrimidin- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) 4- ppm 8.40-8.87 (m, 5H) 7.33-7.47 (m, 3H) 6.91 (d, m/e 445 ylcarbonyl)piperidin- J = 8.85 Hz, 2H) 4.79 (d, J = 7.93 Hz, 4H) 4.48-4.63 (M + H)⁺ 4-yl]oxy}phenyl)- (m, 1H) 3.45-4.22 (m, 4H) 1.94-2.12 (m, 2H) 1.56- 1,3-dihydro-2H- 1.79 (m, 2H) pyrrolo[3,4- c]pyridine-2- carboxamide 1437 N-[4-({1-[(5- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) methylpyrazin-2- ppm 8.66 (s, 1H) 8.57 (s, 1H) 8.52 (s, 1H) 8.48 (d, m/e 459 yl)carbonyl]piperidin- J = 4.88 Hz, 1H) 7.40 (d, J = 8.54 Hz, 3H) 6.91 (d, (M + H)⁺ 4-yl}oxy)phenyl]- J = 9.16 Hz, 2H) 4.79 (d, J = 7.63 Hz, 4H) 4.51-4.60 1,3-dihydro-2H- (m, 1H) 3.63-4.07 (m, 2H) 3.39-3.62 (m, 2H) 2.55 pyrrolo[3,4- (s, 3H) 1.93-2.06 (m, 2H) 1.62-1.78 (m, J = 10.38 c]pyridine-2- Hz, 2H) carboxamide 1438 N-[4-({1-[3- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) (piperidin-1- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.33-7.45 m/e 478 yl)propanoyl]piperidin- (m, 3H) 6.89 (d, J = 8.85 Hz, 2H) 4.79 (d, J = 7.93 Hz, (M + H)⁺ 4-yl}oxy)phenyl]- 4H) 4.43-4.52 (m, 1H) 3.66-3.92 (m, 2H) 3.34- 1,3-dihydro-2H- 3.40 (m, 2H) 2.55-2.62 (m, J = 7.02, 7.02 Hz, 2H) pyrrolo[3,4- 2.46-2.50 (m, 2H) 2.37-2.43 (m, 4H) 1.91-2.00 c]pyridine-2- (m, 2H) 1.55-1.68 (m, 2H) 1.45-1.55 (m, 4H) 1.33- carboxamide 1.42 (m, 2H) 1439 N-(4-{[1- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) (morpholin-4- ppm 8.57 (s, 1H) 8.48 (d, J = 5.19 Hz, 1H) 7.34-7.48 m/e 466 ylacetyl)piperidin-4- (m, 3H) 6.90 (d, J = 8.85 Hz, 2H) 4.79 (d, J = 7.63 Hz, (M + H)⁺ yl]oxy}phenyl)-1,3- 4H) 4.40-4.59 (m, 1H) 3.72-3.91 (m, 2H) 3.53- dihydro-2H- 3.64 (m, 4H) 3.35-3.45 (m, 2H) 3.16 (s, 2H) 2.39- pyrrolo[3,4- 2.47 (m, 4H) 1.90-2.01 (m, 2H) 1.50-1.68 (m, 2H) c]pyridine-2- carboxamide 1440 N-[4-({1-[3-(4- ¹H NMR (400 MHz, DMSO-D₂O, Temp = 90° C.) δ (APCI(+)) methylpiperazin-1- ppm 8.57 (s, 1H) 8.48 (d, J = 4.88 Hz, 1H) 7.36-7.44 m/e 493 yl)propanoyl]piperidin- (m, 3H) 6.89 (d, J = 8.85 Hz, 2H) 4.79 (d, J = 7.93 Hz, (M + H)⁺ 4-yl}oxy)phenyl]- 4H) 4.40-4.60 (m, 1 H) 3.69-3.85 (m, 2H) 3.36- 1,3-dihydro-2H- 3.50 (m, 2H) 2.55-2.63 (m, 2H) 2.46-2.50 (m, 2H) pyrrolo[3,4- 2.40-2.45 (m, 4H) 2.30-2.36 (m, 4H) 2.16 (s, 3H) c]pyridine-2- 1.91-2.00 (m, 2H) 1.52-1.67 (m, 2H) carboxamide 1532 N-(4-{[(3R)-1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.49 (ESI(+)) methylbutanoyl)pyr- (d, J = 5.0 Hz, 1H), 8.28 (s, 1H), 7.49-7.36 (m, 3H), m/e 409 rolidin-3- 6.95-6.79 (m, 2H), 4.96 (d, J = 21.2 Hz, 1H), 4.78 (M + H)⁺ yl]oxy}phenyl)-1,3- (d, J = 4.0 Hz, 5H), 3.81-3.44 (m, 4H), 2.21-1.84 dihydro-2H- (m, 6H), 0.99-0.79 (m, 6H) pyrrolo[3,4- c]pyridine-2- carboxamide 1533 N-(4-{[(3R)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.49 (ESI(+)) (cyclobutylcarbonyl) (d, J = 5.0 Hz, 1H), 8.28 (s, 1H), 7.53-7.38 (m, 3H), m/e 407 pyrrolidin-3- 6.96-6.81 (m, 2H), 5.04-4.85 (m, 1H), 4.78 (d, J = (M + H)⁺ yl]oxy}phenyl)-1,3- 3.9 Hz, 4H), 3.72-3.07 (m, 5H), 2.24-1.56 (m, 8H) dihydro-2H- pyrrolo[3,4- c]pyridine-2- carboxamide 1534 N-[4-({(3R)-1-[(2R)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) tetrahydrofuran-2- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.48-7.43 (m, 2H), m/e 423 ylcarbonyl]pyrrolidin- 7.45-7.39 (m, 2H), 6.92-6.83 (m, 2H), 5.05-4.90 (M + H)⁺ 3-yl}oxy)phenyl]- (m, 1H), 4.82-4.75 (m, 4H), 4.59-4.42 (m, 1H), 1,3-dihydro-2H- 3.89-3.42 (m, 5H), 2.25-1.68 (m, 6H) pyrrolo[3,4- c]pyridine-2- carboxamide 1535 N-[4-({(3R)-1-[(2S)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) tetrahydrofuran-2- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.45-7.39 (m, 2H), m/e 423 ylcarbonyl]pyrrolidin- 6.93-6.83 (m, 2H), 5.06-4.90 (m, 1H), 4.82-4.75 (M + H)⁺ 3-yl}oxy)phenyl]- (m, 4H), 4.60-4.42 (m, 1H), 3.85-3.63 (m, 3H), 1,3-dihydro-2H- 3.63-3.41 (m, 2H), 2.30-1.71 (m, 6H) pyrrolo[3,4- c]pyridine-2- carboxamide 1536 N-(4-{[(3R)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) (cyclopropylacetyl)pyr- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.48-7.40 (m, 3H), m/e 407 rolidin-3- 6.92-6.82 (m, 2H), 5.03-4.90 (m, 1H), 4.81-4.75 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 4H), 3.79-3.43 (m, 2H), 2.32-1.95 (m, 5H), dihydro-2H- 1.05-0.88 (m, 1H), 0.49-0.36 (m, 2H), 0.20-0.07 pyrrolo[3,4- (m, 2H) c]pyridine-2- carboxamide 1537 N-(4-{[(3S)-1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) methylbutanoyl)pyr- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.49-7.39 (m, 3H), m/e 409 rolidin-3- 6.92-6.81 (m, 2H), 5.04-4.89 (m, 1H), 4.81-4.75 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 4H), 3.66-3.42 (m, 4H), 2.25-1.90 (m, 5H), dihydro-2H- 0.96-0.82 (m, 6H) pyrrolo[3,4- c]pyridine-2- carboxamide 1538 N-(4-{[(3S)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) (cyclobutylcarbonyl) (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.48-7.40 (m, 3H), m/e 407 pyrrolidin-3- 6.91-6.81 (m, 2H), 5.02-4.89 (m, 1H), 4.81-4.75 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 4H), 3.32 (s, 5H), 2.27-1.65 (m, 8H) dihydro-2H- pyrrolo[3,4- c]pyridine-2- carboxamide 1539 N-[4-({(3S)-1-[(2R)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) tetrahydrofuran-2- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.48-7.41 (m, 3H), m/e 423 ylcarbonyl]pyrrolidin- 7.43 (d, J = 5 .4 Hz, 2H), 6.93-6.82 (m, 2H), 5.05- (M + H)⁺ 3-yl}oxy)phenyl]- 4.91 (m, 1H), 4.81-4.75 (m, 4H), 4.60-4.42 (m, 1,3-dihydro-2H- 1H), 3.89-3.64 (m, 4H), 3.65-3.43 (m, 2H), 2.26- pyrrolo[3,4- 1.73 (m, 6H) c]pyridine-2- carboxamide 1540 N-[4-({(3S)-1-[(2S)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) tetrahydrofuran-2- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.48-7.40 (m, 3H), m/e 423 ylcarbonyl]pyrrolidin- 6.93-6.83 (m, 2H), 5.05-4.91 (m, 1H), 4.81-4.75 (M + H)⁺ 3-yl}oxy)phenyl]- (m, 3H), 4.59-4.42 (m, 1H), 3.89-3.42 (m, 6H), 1,3-dihydro-2H- 2.25-1.70 (m, 6H) pyrrolo[3,4- c]pyridine-2- carboxamide 1541 N-(4-{[(3S)-1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (ESI(+)) (cyclopropylacetyl)pyr- (d, J = 5.0 Hz, 1H), 8.29 (s, 1H), 7.48-7.40 (m, 3H), m/e 407 rolidin-3- 6.93-6.82 (m, 2H), 5.03-4.90 (m, 1H), 4.81-4.75 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 4H), 3.80-3.33 (m, 2H), 2.30-1.95 (m, 5H), dihydro-2H- 1.07-0.88 (m, 1H), 0.49-0.35 (m, 2H), 0.19-0.07 pyrrolo[3,4- (m, 2H) c]pyridine-2- carboxamide

Example 953 N-{6-[(1-acetylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 953A tert-butyl 4-(5-nitropyridin-2-yloxy)piperidine-1-carboxylate

A suspension of pre-washed NaH (0.1 g, 2.48 mmol, 60% percent dispersion in mineral oil) in THF (2 mL) was added to an ice cold solution of 4-hydroxy-piperidine-1-carboxylic acid tert-butyl ester (0.5 g, 2.48 mmol) in dry THF (3 mL). The mixture was stirred for 20 minutes, and added to 2-chloro-5-nitro-pyridine (0.36 g, 2.26 mmol) in portions. After the addition was completed, the cooling bath was removed and the reaction mixture was stirred at 22° C. overnight. The reaction mixture was cooled in an ice bath and treated with a saturated aqueous sodium bicarbonate solution (5 mL). The reaction mixture was diluted with ethyl acetate (25 mL) and distilled water (25 mL). The separated aqueous phase was extracted with ethyl acetate (3×35 mL), and the combined organic phases were dried over sodium sulfate, filtered and concentrated under reduced pressure. Chromatography provided the title compound.

Example 953B tert-butyl 4-(5-aminopyridin-2-yloxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 274, substituting tert-butyl 4-(5-nitropyridin-2-yloxy)piperidine-1-carboxylate for 5-nitro-N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide.

Example 953C tert-butyl 4-(5-(isoindoline-2-carboxamido)pyridin-2-yloxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(5-aminopyridin-2-yloxy)piperidine-1-carboxylate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.

Example 953D N-(6-(piperidin-4-yloxy)pyridin-3-yl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(5-(isoindoline-2-carboxamido)pyridin-2-yloxy)piperidine-1-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 953E N-{6-[(1-acetylpiperidin-4-yl)oxy]pyridin-3-yl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(6-(piperidin-4-yloxy)pyridin-3-yl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and acetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.37 (s, 1H), 8.26 (d, J=2.7 Hz, 1H), 7.86 (dd, J=8.9, 2.7 Hz, 1H), 7.44-7.24 (m, 4H), 6.75 (d, J=8.8 Hz, 1H), 5.21-5.07 (m, 1H), 4.75 (s, 4H), 3.72-3.63 (m, 1H), 3.40-3.11 (m, 2H), 1.97-1.85 (m, 1H), 1.73-1.38 (m, 2H); MS (ESI(+)) m/e 495 (M+H)⁺.

TABLE 17 The following Examples were essentially prepared as described in Example 1C, substituting N-(6-(piperidin-4-yloxy)pyridin-3-yl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 954 N-{6-[(1- 1H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 8.26 (ESI(+)) isobutyrylpiperidin-4- (dd, J = 2.7, 0.7 Hz, 1H), 7.86 (dd, J = 8.8, 2.7 Hz, m/e 409 yl)oxy]pyridin-3-yl}- 1H), 7.41-7.26 (m, 4H), 6.74 (d, J = 8.5 Hz, 1H), (M + H)⁺ 1,3-dihydro-2H- 5.21-5.09 (m, 1H), 4.75 (s, 4H), 3.99-3.72 (m, 2H), isoindole-2- 3.44-3.14 (m, 2H), 2.98-2.80 (m, 1H), 2.07-1.87 carboxamide (m, 2H), 1.67-1.42 (m, 2H), 1.00 (d, J = 6.7 Hz, 6H) 955 N-(6-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 8.26 (ESI(+)) methylbutanoyl)piperidin- (d, J = 2.9 Hz, 1H), 7.85 (dd, J = 8.8, 2.7 Hz, 1H), m/e 423 4-yl]oxy}pyridin-3- 7.41-7.26 (m, 4H), 6.74 (d, J = 8.8 Hz, 1H), 5.21- (M + H)⁺ yl)-1,3-dihydro-2H- 5.09 (m, 1H), 4.75 (s, 4H), 3.99-3.88 (m, 1H), 3.80- isoindole-2- 3.67 (m, 1H), 3.45-3.13 (m, 3H), 2.22 (d, J = 1.4 Hz, carboxamide 1H), 2.05-1.87 (m, 3H), 1.65-1.41 (m, 2H), 0.91 (d, J = 6.6 Hz, 6H) 956 N-(6-{[1-(4,4,4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 8.26 (ESI(+)) trifluorobutanoyl)piperidin- (d, J = 2.7 Hz, 1H), 7.86 (dd, J = 8.8, 2.7 Hz, 1H), m/e 463 4-yl]oxy}pyridin-3- 7.42-7.26 (m, 4H), 6.75 (d, J = 8.8 Hz, 1H), 5.21- (M + H)⁺ yl)-1,3-dihydro-2H- 5.09 (m, 1H), 4.75 (s, 4H), 3.98-3.85 (m, 1H), 3.77- isoindole-2- 3.66 (m, 1H), 3.42-3.15 (m, 2H), 2.68-2.56 (m, carboxamide 2H), 2.03-1.88 (m, 2H), 1.71-1.41 (m, 2H) 957 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 8.26 (ESI(+)) (methoxyacetyl)piperidin- (d, J = 2.6 Hz, 1H), 7.86 (dd, J = 8.9, 2.7 Hz, 1H), m/e 411 4-yl]oxy}pyridin-3- 7.34 (tdd, J = 9.0, 5.6, 3.5 Hz, 4H), 6.75 (d, J = 8.8 (M + H)⁺ yl)-1,3-dihydro-2H- Hz, 1H), 5.25-5.06 (m, 1H), 4.75 (s, 4H), 4.08 (t, J = isoindole-2- 6.0 Hz, 3H), 3.63 (s, 1H), 3.42-3.11 (m, 5H), 1.96 (s, carboxamide 2H), 1.59 (d, J = 25.8 Hz, 2H) 958 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.38 (s, 1H), 8.26 (ESI(+)) (tetrahydrofuran-2- (d, J = 2.7 Hz, 1H), 7.86 (dd, J = 8.8, 2.7 Hz, 1H), m/e 437 ylcarbonyl)piperidin-4- 7.40-7.28 (m, 4H), 6.75 (d, J = 8.8 Hz, 1H), 5.15 (d, (M + H)⁺ yl]oxy}pyridin-3-yl)- J = 4.1 Hz, 1H), 4.75 (s, 3H), 4.73-4.63 (m, 1H), 1,3-dihydro-2H- 3.92-3.63 (m, 5H), 3.62-3.12 (m, 2H), 2.09-1.89 isoindole-2- (m, 2H), 1.89-1.69 (m, 1H), 1.70-1.32 (m, 1H) carboxamide 959 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.38 (s, 1H), 8.26 (ESI(+)) (tetrahydrofuran-3- (d, J = 2.7 Hz, 1H), 7.86 (dd, J = 8.8, 2.8 Hz, 1H), m/e 437 ylcarbonyl)piperidin-4- 7.40-7.22 (m, 4H), 6.75 (d, J = 8.8 Hz, 1H), 5.16 (M + H)⁺ yl]oxy}pyridin-3-yl)- (dq, J = 8.2, 4.1 Hz, 1H), 4.75 (bs, 4H), 3.98-3.70 1,3-dihydro-2H- (m, 4H), 3.74-3.63 (m, 2H), 3.45-3.14 (m, 3H), isoindole-2- 2.08-1.88 (m, 4H), 1.68-1.43 (m, 2H) carboxamide 960 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.39 (d, J = 8.2 Hz, (ESI(+)) (cyclopropylcarbonyl)piperidin- 1H), 8.31-8.20 (m, 1H), 7.91-7.78 (m, 1H), 7.44- m/e 407 4-yl]oxy}pyridin-3-yl)- 7.24 (m, 4H), 6.82-6.68 (m, 1H), 5.27-5.07 (m, (M + H)⁺ 1,3-dihydro-2H- 1H), 4.75 (s, 4H), 4.07-3.86 (m, 2H), 3.61-3.46 (m, isoindole-2- 1H), 3.26-3.13 (m, 1H), 2.10-1.86 (m, 3H), 1.70- carboxamide 1.42 (m, 2H), 0.79-0.62 (m, 4H) 961 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.38 (s, 1H), 8.26 (ESI(+)) (cyclopropylacetyl)piperidin- (d, J = 3.1 Hz, 1H), 7.86 (dd, J = 8.9, 2.9 Hz, 1H), m/e 421 4-yl]oxy}pyridin-3- 7.43-7.22 (m, 4H), 6.74 (d, J = 8.4 Hz, 1H), 5.21- (M + H)⁺ yl)-1,3-dihydro-2H- 5.09 (m, 1H), 4.75 (bs, 4H), 3.98-3.87 (m, 1H), 3.76- isoindole-2- 3.64 (m, 1H), 3.38-3.14 (m, 2H), 2.28 (d, J = 6.7 carboxamide Hz, 2H), 2.21-1.89 (m, 2H), 1.67-1.43 (m, 2H), 1.05-0.87 (m, 1H), 0.51-0.35 (m, 2H), 0.22-0.08 (m, 2H) 962 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 8.24 (ESI(+)) (cyclobutylcarbonyl)piperidin- (t, J = 4.4 Hz, 1H), 7.93-7.77 (m, 1H), 7.44-7.24 m/e 421 4-yl]oxy}pyridin- (m, 4H), 6.74 (t, J = 6.5 Hz, 1H), 5.23-5.03 (m, 1H), (M + H)⁺ 3-yl)-1,3-dihydro-2H- 4.75 (s, 4H), 3.98-3.81 (m, 1H), 3.66-3.50 (m, 1H), isoindole-2- 3.27-3.10 (m, 2H), 2.26-1.99 (m, 4H), 1.99-1.80 carboxamide (m, 3H), 1.80-1.42 (m, 3H) 963 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.38 (s, 1H), 8.26 (ESI(+)) (cyclopentylcarbonyl)piperidin- (d, J = 2.7 Hz, 1H), 7.85 (dd, J = 8.8, 2.7 Hz, 1H), m/e 435 4-yl]oxy}pyridin-3-yl)- 7.40-7.28 (m, 4H), 6.74 (d, J = 8.8 Hz, 1H), 5.21- (M + H)⁺ 1,3-dihydro-2H- 5.09 (m, 1H), 4.75 (s, 4H), 3.98-3.75 (m, 3H), 3.45- isoindole-2- 3.31 (m, 1H), 3.26-3.14 (m, 1H), 3.00 (p, J = 7.6 Hz, carboxamide 1H), 2.03-1.87 (m, 2H), 1.81-1.44 (m, 10H) 964 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 8.26 (ESI(+)) (cyclopentylacetyl)piperidin- (dd, J = 2.7, 0.7 Hz, 1H), 7.85 (dd, J = 8.8, 2.7 Hz, m/e 449 4-yl]oxy}pyridin-3- 1H), 7.41-7.26 (m, 4H), 6.74 (d, J = 8.5 Hz, 1H), (M + H)⁺ yl)-1,3-dihydro-2H- 5.20-5.08 (m, 1H), 4.75 (s, 3H), 3.99-3.86 (m, 1H), isoindole-2- 3.79-3.68 (m, 1H), 3.25-3.05 (m, 1H), 2.36 (d, J = carboxamide 0.8 Hz, 1H), 2.35-2.06 (m, 3H), 2.04-1.85 (m, 2H), 1.82-1.68 (m, 2H), 1.65-1.40 (m, 6H), 1.23-0.99 (m, 2H) 965 N-(6-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 8.26 (ESI(+)) (cyclohexylcarbonyl)piperidin- (d, J = 2.3 Hz, 1H), 7.85 (dd, J = 8.8, 2.7 Hz, 1H), m/e 449 4-yl]oxy}pyridin- 7.33 (s, 2H), 6.74 (d, J = 8.8 Hz, 1H), 5.21-5.09 (m, (M + H)⁺ 3-yl)-1,3-dihydro-2H- 1H), 4.75 (s, 4H), 3.99-3.72 (m, 2H), 3.25-3.11 (m, isoindole-2- 1H), 2.56 (d, J = 19.6 Hz, 1H), 2.06-1.85 (m, 2H), carboxamide 1.74-1.08 (m, 13H)

Example 966 tert-butyl (2-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}ethyl)carbamate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-aminophenethylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), 7.50-7.43 (m, 2H), 7.40-7.26 (m, 4H), 7.11-7.03 (m, 2H), 6.87-6.79 (m, 1H), 4.75 (s, 4H), 3.18-3.02 (m, 2H), 2.66-2.58 (m, 2H), 1.37 (s, 9H); MS (ESI(+)) m/e 382 (M+H)⁺.

Example 973 N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 808, substituting (tetrahydrofuran-3-yl)methanamine for 3-methylbutan-1-amine in Example 808A. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.76 (s, 1H), 7.82-7.75 (m, 2H), 7.71-7.64 (m, 2H), 7.54 (t, J=6.1 Hz, 1H), 7.41-7.25 (m, 4H), 4.80 (bs, 4H), 3.70-3.49 (m, 3H), 2.69 (t, J=6.7 Hz, 2H), 2.34-2.16 (m, 1H), 1.94-1.79 (m, 1H), 1.54-1.39 (m, 1H); MS (ESI(+)) m/e 402 (M+H)⁺.

Example 974 N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-amino-N-((tetrahydrofuran-3-yl)methyl)benzenesulfonamide for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.83 (s, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 7.82-7.75 (m, 2H), 7.72-7.65 (m, 2H), 7.55 (t, J=6.0 Hz, 1H), 7.44 (d, J=5.1 Hz, 1H), 4.87-4.75 (m, 4H), 3.76-3.49 (m, 3H), 2.69 (t, J=6.7 Hz, 2H), 2.34-2.16 (m, 1H), 1.94-1.79 (m, 1H), 1.54-1.39 (m, 1H); MS (ESI(+)) m/e 403 (M+H)⁺.

Example 975 5-cyano-N-{4-[(tetrahydrofuran-3-ylmethyl)sulfamoyl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-amino-N-((tetrahydrofuran-3-yl)methyl)benzenesulfonamide for 4-amino-N-propylbenzamide and isoindoline-5-carbonitrile for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.83 (s, 1H), 7.89 (s, 1H), 7.83-7.74 (m, 3H), 7.72-7.64 (m, 2H), 7.59 (d, J=7.9 Hz, 1H), 7.54 (t, J=6.1 Hz, 1H), 4.93-4.76 (m, 4H), 3.70-3.49 (m, 3H), 2.69 (t, J=6.7 Hz, 2H), 2.31-2.05 (m, 1H), 1.94-1.78 (m, 1H), 1.54-1.39 (m, 1H); MS (ESI(+)) m/e 427 (M+H)⁺.

Example 979 N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 979A N-(4-(piperidin-4-yl)phenyl)isoindoline-2-carboxamide

tert-Butyl 4-(4-(isoindoline-2-carboxamido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate (1.00 g, 2.38 mmol) in 20 ml of 1:1 methanol/tetrahydrofuran was added to 5% Pd on carbon (wet) (0.200 g) in a 50 ml pressure bottle and stirred for 16 hours at 30 atm and room temperature. The mixture was filtered through a nylon membrane and concentrated. The residue was suspended in dichloromethane, stirred 1 hour and filtered with dichloromethane washes to provide the title compound.

Example 979B N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(piperidin-4-yl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and tetrahydrofuran-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), 7.46 (m, 2H), 7.31 (m, 4H), 7.12 (m, 2H), 4.74 (bs, 4H), 4.53 (m, 1H), 4.05 (m, 1H), 3.87 (m, 1H), 3.70 (m, 3H), 3.36 (m, 2H), 3.12 (m, 1H), 2.75-2.58 (m, 1H), 2.01 (m, 2H), 1.76 (m, 2H), 1.45 (m, 2H); MS (ESI(+)) m/e 420 (M+H).

TABLE 18 The following Examples were essentially prepared as described in Example 1C, substituting the apropriate amine for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 980 N-{4-[1-(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (d, J = (ESI(+)) 2-ylcarbonyl)piperidin-4- 8.7 Hz, 1H), 7.47 (m, 2H), 7.33 (m, 4H), 7.14 (m, m/e 420 yl]phenyl}-1,3-dihydro- 2H), 4.75 (s, 4H), 4.68 (m, 1H), 4.45 (m, 1H), 4.09 (M + H)⁺ 2H-isoindole-2- (m, 1H), 3.75 (m, 2H), 3.10 (m, 1H), 2.76-2.56 (m, carboxamide 2H), 2.04 (m, 2H), 1.80 (m, 4H), 1.61-1.33 (m, 2H) 981 N-{4-[1-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), (ESI(+)) pyran-4- 7.47 (m, 2H), 7.33 (m, 4H), 7.12 (m, 2H), 4.75 (bs, m/e 434 ylcarbonyl)piperidin-4- 4H), 4.55 (m, 1H), 4.09 (m, 1H), 3.85 (m, 2H), 3.40 (M + H)⁺ yl]phenyl}-1,3-dihydro- (m, 2H), 3.09 (m, 1H), 2.91 (m, 1H), 2.70 (m, 1H), 2H-isoindole-2- 2.56 (m, 1H), 1.79 (m, 2H), 1.68-1.35 (m, 6H) carboxamide 982 N-{4-[1-(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), (ESI(+)) ylcarbonyl)piperidin-4- 7.48 (t, J = 1 0.0 Hz, 2H), 7.32 (m, 4H), 7.10 (d, J = m/e 436 yl]phenyl}-1,3-dihydro- 7.5 Hz, 2H), 4.74 (s, 4H), 4.44 (d, J = 12.2 Hz, 1H), (M + H)⁺ 2H-isoindole-2- 4.34 (t, J = 9.2 Hz, 1H), 4.07 (d, J = 11.4 Hz, 1H), carboxamide 3.83-3.56 (m, 4H), 3.50 (m, 2H), 3.08 (m, 1H), 2.66 (m, 2H), 1.78 (m, 2H), 1.67-1.30 (m, 2H) 983 N-(4-{1-[(1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), (ESI(+)) methylpyrrolidin-3- 7.46 (d, J = 8.3 Hz, 2H), 7.31 (m, 4H), 7.11 (d, J = m/e 433 yl)carbonyl]piperidin-4- 8.3 Hz, 2H), 4.74 (s, 4H), 4.52 (d, J = 12.0 Hz, 1H), (M + H)⁺ yl}phenyl)-1,3-dihydro- 4.01 (d, J = 13.0 Hz, 1H), 3.25 (m, 1H), 3.06 (m, 2H-isoindole-2- 1H), 2.71 (m, 2H), 2.63-2.43 (m, 3H), 2.32 (m, carboxamide 1H), 2.21 (s, 3H), 1.94 (m, 2H), 1.75 (m, 2H), 1.59- 1.30(m, 2H) 984 N-(4-{1-[(1,1- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.27 (s, 1H), (ESI(+)) dioxidotetrahydrothiophen-3- 7.48 (m, 2H), 7.31 (m, 4H), 7.14 (m, 2H), 4.75 (s, m/e 468 yl)carbonyl]piperidin-4- 4H), 4.53 (m, 1H), 4.08 (m, 1H), 3.75 (m, 1H), 3.30- (M + H)⁺ yl}phenyl)-1,3-dihydro- 3.04 (m, 5H), 2.71 (m, 2H), 2.33 (m, 1H), 2.08 (m, 2H-isoindole-2- 1H), 1.79 (m, 2H), 1.66-1.36 (m, 2H) carboxamide 985 N-{4-[1-(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), (ESI(+)) methylpropanoyl)piperidin- 7.48 (m, 2H), 7.31 (m, 4H), 7.11 (d, J = 8.5 Hz, 2H), m/e 408 4-yl]phenyl}-1,3- 5.37 (s, 1H), 4.74 (s, 4H), 4.53 (m, 2H), 3.30 (m, (M + H)⁺ dihydro-2H-isoindole-2- 1H), 2.71 (m, 2H), 1.76 (d, J = 11.8 Hz, 2H), 1.50 carboxamide (m, 2H), 1.32 (s, 6H) 986 N-{4-[1-(morpholin-4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.26 (s, 1H), (ESI(+)) ylacetyl)piperidin-4- 7.46 (m, 2H), 7.33 (m, 4H), 7.10 (m, 2H), 4.74 (bs, m/e 449 yl]phenyl}-1,3-dihydro- 4H), 4.46 (m, 1H), 4.13 (m, 1H), 3.57 (m, 4H), 3.06 (M + H)⁺ 2H-isoindole-2- (m, 3H), 2.71-2.50 (m, 2H), 2.40 (m, 4H), 1.77 (m, carboxamide 2H), 1.56 (m, 1H), 1.40 (m, 1H) 1469 N-(4-{1-[(2R)- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.28 (s, 1H), (ESI(+)) tetrahydrofuran-2- 7.47 (m, 2H), 7.32 (m, 4H), 7.13 (m, 2H), 4.75 (s, m/e 420 ylcarbonyl]piperidin-4- 4H), 4.70 (m, 1H), 4.48 (m, 1H), 4.10 (m, 1H), 3.76 (M + H)⁺ yl}phenyl)-1,3-dihydro- (m, 2H), 3.08 (m, 1H), 2.69 (m, 2H), 2.03 (m, 2H), 2H-isoindole-2- 1.81 (m, 4H), 1.54 (m, 1H), 1.42 (m, 1H) carboxamide 1470 N-(4-{1-[(2S)- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.28 (s, 1H), (ESI(+)) tetrahydrofuran-2- 7.47 (m, 2H), 7.33 (m, 4H), 7.12 (dd, J = 8.3, 2.5 Hz, m/e 420 ylcarbonyl]piperidin-4- 2H), 4.75 (s, 4H), 4.68 (dd, J = 7.5, 5.7 Hz, 1H), 4.49 (M + H)⁺ yl}phenyl)-1,3-dihydro- (m, 1H), 4.10 (m, 1H), 3.76 (m, 2H), 3.13 (m, 1H), 2H-isoindole-2- 268 (m, 2H), 2.01 (m, 2H), 1.80 (m, 4H), 1.50 (m, 2H) carboxamide 1471 N-(4-{1-[(3R)- A-1361467.0 - ¹H NMR (400 MHz, DMSO-d₆) δ (ESI(+)) tetrahydrofuran-3- 8.28 (s, 1H), 7.47 (m, 2H), 7.34 (m, 4H), 7.13 (m, m/e 420 ylcarbonyl]piperidin-4- 2H), 4.75 (s, 4H), 4.54 (m, 1H), 4.08 (m, 1H), 3.88 (M + H)⁺ yl}phenyl)-1,3-dihydro- (m, 1H), 3.71 (m, 3H), 3.39 (m, 1H), 3.14 (m, 1H), 2H-isoindole-2- 2.66 (m, 2H), 2.01 (m, 2H), 1.79 (m, 2H), 1.46 (m, 2H) carboxamide

Example 1013 N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 1013A tert-butyl 4-(4-(isoindoline-2-carboxamido)phenoxy)piperidine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(4-aminophenoxy)piperidine-1-carboxylate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.

Example 1013B N-(4-(piperidin-4-yloxy)phenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(isoindoline-2-carboxamido)phenoxy)piperidine-1-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1013C N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(piperidin-4-yloxy)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and tetrahydrofuran-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.20 (s, 1H), 7.47-7.27 (m, 6H), 6.93-6.86 (m, 2H), 4.74 (s, 4H), 4.58-4.47 (m, 1H), 3.93-3.56 (m, 6H), 3.44-3.32 (m, 3H), 2.06-1.83 (m, 4H), 1.69-1.40 (m, 2H); MS (ESI(+)) m/e 436 (M+H)⁺.

TABLE 19 The following Examples were essentially prepared as described in Example 1C, substituting an appropriate amine for 3-phenylpropan-1-amine and appropriate acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 1028 N-(4-{[1-(2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.20 (s, 1H), 7.42 (ESI(+)) methylbutanoyl)piperidin- (dd, J = 12.5, 10.6 Hz, 2H), 7.37-7.23 (m, 4H), 6.90 m/e 422 4-yl]oxy}phenyl)-1,3- (d, J = 9.0 Hz, 2H), 4.74 (s, 4H), 4.66-4.42 (m, 1H), (M + H)⁺ dihydro-2H-isoindole-2- 3.90 (s, 2H), 3.45-3.11 (m, 2H), 2.73 (dd, J = 13.4, carboxamide 6.8 Hz, 1H), 1.92 (s, 2H), 1.68-1.12 (m, 4H), 0.98 (d, J = 6.7 Hz, 3H), 0.81 (t, J = 7.4 Hz, 3H) 1029 N-(4-{[1-(3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.19 (s, 1H), 7.48- (ESI(+)) methylbutanoyl)piperidin- 7.38 (m, 2H), 7.33 (tdd, J = 8.9, 5.6, 3.5 Hz, 4H), 6.98- m/e 422 4-yl]oxy}phenyl)-1,3- 6.81 (m, 2H), 4.74 (s, 4H), 4.50 (dt, J = 8.0, 4.1 Hz, (M + H)⁺ dihydro-2H-isoindole-2- 1H), 3.85 (s, 1H), 3.69 (s, 1H), 3.21 (d, J = 9.3 Hz, carboxamide 1H), 2.34-2.14 (m, 2H), 2.13-1.80 (m, 3H), 1.53 (d, J = 21.1 Hz, 2H), 0.90 (d, J = 6.6 Hz, 6H) 1030 N-(4-{[1-(2,3- ¹H NMR (300 MHz, DMSO-d₆) δ 8.20 (s, 1H), 7.47- (ESI(+)) dimethylbutanoyl)piperidin- 7.27 (m, 6H), 6.94-6.86 (m, 2H), 4.74 (s, 4H), 4.72- m/e 436 4-yl]oxy}phenyl)- 4.47 (m, 1H), 4.02-3.76 (m, 2H), 3.50-3.12 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 2.00-1.63 (m, 3H), 1.63-1.39 (m, 2H), 0.95 isoindole-2- (d, J = 6.7 Hz, 3H), 0.85 (t, J = 6.6 Hz, 6H) carboxamide 1031 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.20 (s, 1H), 7.44 (ESI(+)) (tetrahydrofuran-2- (d, J = 9.0 Hz, 2H), 7.34 (tdd, J = 8.9, 5.5, 3.5 Hz, m/e 436 ylcarbonyl)piperidin-4- 4H), 6.90 (d, J = 9.0 Hz, 2H), 4.74 (s, 4H), 4.70-4.63 (M + H)⁺ yl]oxy}phenyl)-1,3- (m, 1H), 4.51 (s, 1H), 3.80-3.68 (m, 4H), 3.47-3.08 dihydro-2H-isoindole-2- (m, 2H), 2.13-1.68 (m, 6H), 1.66-1.33 (m, 2H) carboxamide 1032 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.18 (d, J = 6.7 Hz, (ESI(+)) (cyclohexylcarbonyl)piperidin- 1H), 7.48-7.39 (m, 2H), 7.39-7.22 (m, 4H), 6.96- m/e 448 4-yl]oxy}phenyl)-1,3- 6.81 (m, 2H), 4.74 (s, 4H), 4.56-4.41 (m, 1H), 3.97- (M + H)⁺ dihydro-2H-isoindole-2- 3.64 (m, 2H), 3.28-3.10 (m, 2H), 2.67-2.54 (m, carboxamide 1H), 2.02-1.78 (m, 2H), 1.74-1.39 (m, 7H), 1.39- 1.04 (m, 5H) 1033 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.20 (s, 1H), 7.41 (ESI(+)) (cyclohexylacetyl)piperidin- (t, J = 11.1 Hz, 2H), 7.37-7.20 (m, 4H), 6.89 (d, J = m/e 462 4-yl]oxy}phenyl)- 9.0 Hz, 2H), 4.74 (s, 4H), 4.57-4.38 (m, 1H), 3.77 (M + H)⁺ 1,3-dihydro-2H- (d, J = 47.0 Hz, 2H), 3.21 (t, J = 9.7 Hz, 2H), 2.20 (d, isoindole-2- J = 6.6 Hz, 2H), 1.89 (s, 2H), 1.60 (t, J = 30.4 Hz, carboxamide 8H), 1.17 (dd, J = 28.3, 16.2 Hz, 3H), 0.94 (t, J = 11.4 Hz, 2H) 1034 N-(4-{[1-(tetrahydro- ¹H NMR (300 MHz, DMSO-d₆) δ 8.20 (s, 1H), 7.40 (ESI(+)) 2H-pyran-4- (dd, J = 19.8, 6.3 Hz, 3H), 7.36-7.23 (m, 3H), 6.89 m/e 464 ylacetyl)piperidin-4- (d, J = 9.0 Hz, 2H), 4.74 (s, 4H), 4.50 (s, 1H), 3.95- (M + H)⁺ yl]oxy}phenyl)-1,3- 3.64 (m, 4H), 3.28-3.14 (m, 4H), 2.27 (d, J = 6.4 Hz, dihydro-2H-isoindole-2- 2H), 1.91 (d, J = 3.7 Hz, 3H), 1.55 (t, J = 18.1 Hz, carboxamide 4H), 1.32-1.07 (m, 2H) 1035 N-(4-{[1-(morpholin-4- ¹H NMR (300 MHz, DMSO-d₆) δ 10.01 (s, 1H), 8.21 (ESI(+)) ylacetyl)piperidin-4- (s, 1H), 7.43 (t, J = 13.2 Hz, 2H), 7.37-7.24 (m, 3H), m/e 465 yl]oxy}phenyl)-1,3- 6.91 (d, J = 9.1 Hz, 2H), 4.74 (s, 4H), 4.71-4.45 (m, (M + H)⁺ dihydro-2H-isoindole-2- 1H), 4.37 (s, 2H), 4.04-3.71 (m, 6H), 3.56 (d, J = carboxamide 15.9 Hz, 2H), 3.47-3.20 (m, 4H), 3.13 (s, 2H), 1.97 (s, 2H), 1.62 (dd, J = 33.2, 8.7 Hz, 2H) 1036 N-(4-{[1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.20 (s, 1H), 7.51- (ESI(+)) (tetrahydrofuran-3- 7.35 (m, 3H), 7.35-7.23 (m, 3H), 6.89 (d, J = 9.0 Hz, m/e 450 ylacetyl)piperidin-4- 2H), 4.74 (s, 4H), 4.50 (dd, J = 7.7, 3.9 Hz, 1H), 3.92- (M + H)⁺ yl]oxy}phenyl)-1,3- 3.71 (m, 3H), 3.71-3.52 (m, 2H), 3.22 (dd, J = 9.8, dihydro-2H-isoindole-2- 4.3 Hz, 3H), 2.45 (s, 3H), 2.13-1.80 (m, 3H), 1.67- carboxamide 1.37 (m, 3ff)

Example 1018 N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1018A N-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

2,3-Dihydro-1H-pyrrolo[3,4-c]pyridine 2.HCl (1.55 g, 8.03 mmol) was suspended in dimethylformamide (30 ml) and treated with triisopropylethylamine (4.21 ml, 24.08 mmol). After stirring for 20 minutes, the mixture was cooled to −15° C. 2-(4-Isocyanatophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (2.028 g, 8.03 mmol) was dissolved in 10 ml tetrahydrofuran and added via syringe over 10 minutes. The mixture was allowed to warm to room temperature, and it was stirred for 3 hours and concentrated under a stream of nitrogen to minimal volume. The residue was diluted with cold water to give a turbid mixture which was filtered with water washes to provide the title compound after drying.

Example 1018B tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)cyclohex-3-enylcarbamate

N-(4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide (1.692 g, 4.63 mmol), 4-(tert-butoxycarbonylamino)cyclohex-1-enyl trifluoromethanesulfonate (1.6 g, 4.63 mmol) and cesium carbonate (3.77 g, 11.58 mmol) were suspended in terahydrofuran (30 ml), methanol (5.00 ml) and water (15.00 ml). Nitrogen was bubbled through the solution for 10 min when PdCl₂(dppf)-dichloromethane adduct (0.189 g, 0.232 mmol) was added and the mixture was heated to 80° C. for 7 h. After dilution with ethyl acetate and brine, the separated aqueous layer was extracted several times with ethyl acetate and the combined organic layers were dried over magnesium sulfate, filtered and concentrated. Flash chromatography provided the title compound.

Example 1018C N-(4-(4-aminocyclohex-1-enyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)cyclohex-3-enylcarbamate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1018D N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and isobutyric acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.41 (s, 1H), 7.66 (d, J=7.6 Hz, 1H), 7.56-7.48 (m, 2H), 7.43 (d, J=5.1 Hz, 1H), 7.37-7.29 (m, 2H), 6.06-5.99 (m, 1H), 4.83-4.77 (m, 4H), 3.87-3.73 (m, 1H), 2.37 (t, J=6.7 Hz, 2H), 2.11-1.97 (m, 1H), 1.95-1.82 (m, 1H), 1.80-1.50 (m, 1H), 1.38-1.20 (m, 2H), 1.00 (dd, J=6.8, 2.5 Hz, 6H); MS (ESI(+)) m/e 405 (M+H)⁺.

TABLE 20 The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex- 1-enyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 1022 N-(4-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) [(tetrahydrofuran-3- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.91 (d, J = 7.5 Hz, 1H), m/e 433 ylcarbonyl)amino]cyclohex- 7.52 (d, J = 8.6 Hz, 2H), 7.43 (d, J = 5.0 Hz, 1H), 7.33 (M + H)⁺ 1-en-1-yl}phenyl)- (d, J = 8.6 Hz, 2H), 6.02 (s, 1H), 4.80 (d, J = 4.1 Hz, 1,3-dihydro-2H- 4H), 3.84 (td, J = 8.1, 3.7 Hz, 2H), 3.76-3.52 (m, pyrrolo[3,4-c]pyridine- 3H), 2.93 (p, J = 7.7 Hz, 1H), 2.11-1.79 (m, 5H), 2-carboxamide 1.60 (s, 1H) 1023 N-(4-{4-[(tetrahydro- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) 2H-pyran-4- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.77-7.69 (m, 1H), 7.56- m/e 447 ylcarbonyl)amino]cyclohex- 7.48 (m, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.37-7.29 (M + H)⁺ 1-en-1-yl}phenyl)- (m, 2H), 6.02 (bs, 1H), 4.84-4.72 (m, 4H), 3.90- 1,3-dihydro-2H- 3.78 (m, 4H), 2.48-2.41 (m, 2H), 2.36 (s, 2H), 2.11- pyrrolo[3,4-c]pyridine- 1.98 (m, 1H), 1.93-1.81 (m, 1H), 1.69-1.52 (m, 6H) 2-carboxamide 1024 N-(4-{4-[(morpholin-4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) ylacetyl)amino]cyclohex- J = 4.9 Hz, 1H), 8.42 (s, 1H), 7.62 (d, J = 8.1 Hz, 1H), m/e 462 1-en-1-yl}phenyl)- 7.53 (d, J = 8.7 Hz, 2H), 7.43 (d, J = 5.0 Hz, 1H), 7.33 (M + H)⁺ 1,3-dihydro-2H- (d, J = 8.7 Hz, 2H), 6.02 (s, 1H), 4.80 (d, J = 4.2 Hz, pyrrolo[3,4-c]pyridine- 4H), 3.91 (s, 1H), 3.64-3.49 (m, 5H), 2.92 (s, 2H), 2-carboxamide 2.41 (dd, J = 12.8, 8.2 Hz, 5H), 2.18 (s, 1H), 1.86 (s, 1H), 1.77-1.59 (m, 1H) 1025 N-[4-(4-{[(2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) methoxyethoxy)acetyl] J = 4.9 Hz, 1H), 8.42 (s, 1H), 7.59-7.49 (m, 3H), 7.43 m/e 451 amino}cyclohex-1-en- (d, J = 5.1 Hz, 1H), 7.37-7.30 (m, 2H), 6.03 (bs, 1H), (M + H)⁺ 1-yl)phenyl]-1,3- 4.83-4.77 (m, 4H), 3.88 (s, 4H), 3.60 (d, J = 3.8 Hz, dihydro-2H- 2H), 3.48 (d, J = 2.8 Hz, 2H), 3.25 (s, 3H), 2.36-1.97 pyrrolo[3,4-c]pyridine- (m, 3H), 1.93-1.82 (m, 1H), 1.77-1.57 (m, 1H) 2-carboxamide 1081 N-(4-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) [(tetrahydrofuran-2- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.79 (d, J = 7.4 Hz, 1H), m/e 447 ylacetyl)amino]cyclohex- 7.52 (d, J = 8.7 Hz, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.33 (M + H)⁺ 1-en-1-yl}phenyl)- (d, J = 8.7 Hz, 2H), 6.02 (s, 1H), 4.80 (d, J = 4.0 Hz, 1,3-dihydro-2H- 4H), 4.07 (p, J = 6.7 Hz, 1H), 3.83 (s, 1H), 3.73 (dd, J = pyrrolo[3,4-c]pyridine- 14.2, 7.3 Hz, 1H), 3.58 (dd, J = 14.5, 7.6 Hz, 1H), 2-carboxamide 2.45 (s, 2H), 2.34 (dd, J = 13.8, 6.9 Hz, 2H), 2.28- 2.16 (m, 1H), 2.11-1.96 (m, 1H), 1.96-1.71 (m, 4H), 1.68-1.39 (m, 2H) 1082 N-(4-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) [(tetrahydrofuran-3- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.84 (d, J = 7.6 Hz, 1H), m/e 447 ylacetyl)amino]cyclohex- 7.52 (d, J = 8.8 Hz, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.36- (M + H)⁺ 1-en-1-yl}phenyl)- 7.29 (m, 2H), 6.02 (bs, 1H), 4.83-4.77 (m, 4H), 1,3-dihydro-2H- 3.91-3.79 (m, 1H), 3.78-3.67 (m, 1H), 3.66-3.55 pyrrolo[3,4-c]pyridine- (m, 1H), 3.26 (q, J = 3.7 Hz, 1H), 2.44 (dd, J = 10.1, 2-carboxamide 4.1 Hz, 2H), 2.41-2.33 (m, 1H), 2.21-2.12 (m, 1H), 2.11-1.82 (m, 4H), 1.67-1.41 (m, 3H) 1083 N-(4-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) [(cyclohexylcarbonyl)ami- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.62 (d, J = 7.6 Hz, 1H), m/e 445 no]cyclohex-1-en-1- 7.56-7.48 (m, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.36- (M + H)⁺ yl}phenyl)-1,3- 7.29 (m, 2H), 6.01 (bs, 1H), 4.83-4.77 (m, 4H), 3.84- dihydro-2H- 3.74 (m, 1H), 2.43-2.29 (m, 2H), 2.29-1.97 (m, pyrrolo[3,4-c]pyridine- 2H), 1.91-1.80 (m, 1H), 1.74-1.48 (m, 6H), 1.43- 2-carboxamide 1.03 (m, 5H) 1084 N-[4-(4-{[(1,1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) dioxidotetrahydrothiophen-3- J = 5.0 Hz, 1H), 8.42 (s, 1H), 8.12 (d, J = 7.4 Hz, 1H), m/e 481 yl)carbonyl]amino}cyclohex- 8.10-8.05 (m, 1H), 7.53 (d, J = 8.8 Hz, 2H), 7.43 (d, (M + H)⁺ 1-en-1- J = 5.1 Hz, 1H), 7.34 (d, J = 8.7 Hz, 2H), 6.02 (s, 1H), yl)phenyl]-1,3-dihydro- 4.80 (d, J = 4.1 Hz, 4H), 3.85 (s, 1H), 3.21 (ddd, J = 2H-pyrrolo[3,4- 16.3, 11.0, 6.6 Hz, 3H), 3.14-2.96 (m, 2H), 2.31 (dd, c]pyridine-2- J = 12.3, 6.1 Hz, 2H), 2.19-1.97 (m, 2H), 1.88 (s, carboxamide 1H), 1.62 (s, 1H) 1085 N-[4-(4-{[(4,4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) difluorocyclohexyl)carbonyl]ami- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.80 (d, J = 7.5 Hz, 1H), m/e 481 no}cyclohex- 7.56-7.48 (m, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.37- (M + H)⁺ 1-en-1-yl)phenyl]-1,3- 7.29 (m, 2H), 6.02 (bs, 1H), 4.83-4.77 (m, 4H), 3.89- dihydro-2H- 3.77 (m, 1H), 2.41 (d, J = 23.9 Hz, 1H), 2.24-2.14 pyrrolo[3,4-c]pyridine- (m, 1H), 2.12-1.96 (m, 4H), 1.80 (d, J = 22.0 Hz, 2-carboxamide 4H), 1.70-1.50 (m, 4H) 1086 N-(4-{4-[(2-hydroxy-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) methylpropanoyl)ami- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.56-7.49 (m, 2H), 7.42 m/e 421 no]cyclohex-1-en-1- (d, J = 3.1 Hz, 2H), 7.37-7.30 (m, 2H), 6.03 (bs, 1H), (M + H)⁺ yl}phenyl)-1,3- 5.38 (s, 1H), 4.84-4.72 (m, 4H), 3.89-3.79 (m, 1H), dihydro-2H- 2.35 (s, 1H), 2.39-2.05 (m, 2H), 1.80 (d, J = 19.6 Hz, pyrrolo[3,4-c]pyridine- 1H), 1.77-1.61 (m, 1H), 1.25 (s, 6H) 2-carboxamide 1087 N-(4-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) [(tetrahydrofuran-2- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.65-7.54 (m, 1H), 7.52 m/e 433 ylcarbonyl)amino]cyclohex- (d, J = 8.7 Hz, 2H), 7.43 (d, J = 5.0 Hz, 1H), 7.33 (d, J = (M + H)⁺ 1-en-1-yl}phenyl)- 8.7 Hz, 2H), 6.02 (s, 1H), 4.80 (d, J = 4.0 Hz, 4H), 1,3-dihydro-2H- 4.20 (dd, J = 8.1, 5.1 Hz, 1H), 3.89 (dd, J = 13.8, 7.1 pyrrolo[3,4-c]pyridine- Hz, 2H), 3.76 (dd, J = 14.4, 6.7 Hz, 1H), 2.30 (dd, J = 2-carboxamide 28.6, 11.2 Hz, 1H), 2.26-2.01 (m, 3H), 1.93-1.60 (m, 6H) 1291 N-(4-{4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) [(cyclopropylacetyl)ami- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.67 (d, J = 7.6 Hz, 1H), m/e 417 no]cyclohex-1-en-1- 7.56-7.49 (m, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.37- (M + H)⁺ yl}phenyl)-1,3- 7.29 (m, 2H), 6.02 (bs, 1H), 4.84-4.77 (m, 4H), 3.92- dihydro-2H- 3.75 (m, 1H), 2.42 (d, J = 23.1 Hz, 2H), 2.10-2.03 pyrrolo[3,4-c]pyridine- (m, 1H), 1.99 (d, J = 7.0 Hz, 2H), 1.94-1.84 (m, 1H), 2-carboxamide 1.83-1.51 (m, 1H), 1.05-0.88 (m, 1H), 0.43(dd, J = 9.8, 4.2 Hz, 2H), 0.21-0.07 (m, 2H) 1442 N-[4-(4-{[(4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) methylpiperazin-1- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.59-7.49 (m, 3H), 7.43 m/e 475 yl)acetyl]amino}cyclohex- (d, J = 4.6 Hz, 1H), 7.37-7.30 (m, 2H), 6.06-5.98 (M + H)⁺ 1-en-1-yl)phenyl]- (m, 1H), 5.75 (s, 1H), 4.84-4.77 (m, 4H), 4.00-3.85 1,3-dihydro-2H- (m, 1H), 3.05-2.90 (m, 2H), 2.90 (s, 3H), 2.32-2.13 pyrrolo[3,4-c]pyridine- (m, 5H), 2.12 (s, 3H), 2.12 (s, 3H), 1.91-1.80 (m, 2-carboxamide 1H), 1.75-1.61 (m, 1H) 1443 N-(4-{4-[(tetrahydro- ¹H NMR (300 MHz, DMSO-d₆) δ 8.65-8.57 (m, 1H), (ESI(+)) 2H-pyran-4- 8.55-8.45 (m, 1H), 8.44-8.36 (m, 2H), 7.88-7.75 m/e 461 ylacetyl)amino]cyclohex- (m, 1H), 7.60-7.47 (m, 2H), 7.47-7.37 (m, 1H), (M + H)⁺ 1-en-1-yl}phenyl)- 7.36-7.24 (m, 2H), 6.07-5.86 (m, 1H), 4.87-4.62 1,3-dihydro-2H- (m, 4H), 3.90-3.68 (m, 2H), 3.29-3.17 (m, 2H), pyrrolo[3,4-c]pyridine- 2.45-2.28 (m, 2H), 2.09-1.91 (m, 4H), 1.93-1.79 2-carboxamide (m, 2H), 1.64-1.42 (m, 3H), 1.28-1.07 (m, 2H) 1444 N-{4-[4- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.49 (t, (ESI(+)) (benzoylamino)cyclohex- J = 4.7 Hz, 1H), 8.43 (s, 1H), 8.32 (d, J = 7.7 Hz, 1H), m/e 439 1-en-1-yl]phenyl}- 7.91-7.83 (m, 2H), 7.57-7.41 (m, 6H), 7.38-7.28 (M + H)⁺ 1,3-dihydro-2H- (m, 2H), 6.07 (d, J = 1.8 Hz, 1H), 4.87-4.71 (m, 4H), pyrrolo[3,4-c]pyridine- 4.16-3.95 (m, 1H), 2.35-2.19 (m, 2H), 2.08-1.93 2-carboxamide (m, 2H), 1.8 1-1.65 (m, 2H) 1445 N-[4-(4-{[(2S)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.62 (d, J = 5.8 Hz, (ESI(+)) tetrahydrofuran-2- 1H), 8.54-8.45 (m, 1H), 8.44-8.35 (m, 1H), 7.63- m/e 433 ylcarbonyl]amino}cyclohex- 7.54 (m, 1H), 7.56-7.46 (m, 2H), 7.46-7.38 (m, (M + H)⁺ 1-en-1- 1H), 7.33 (d, J = 8.7 Hz, 2H), 6.06-5.90 (m, 1H), yl)phenyl]-1,3-dihydro- 4.86-4.65 (m, 4H), 4.26-4.11 (m, 1H), 3.94-3.80 2H-pyrrolo[3,4- (m, 2H), 3.80-3.62 (m, 1H), 2.40-2.25 (m, 2H), c]pyridine-2- 2.27-2.02 (m, 2H), 1.92-1.77 (m, 4H), 1.75-1.60 carboxamide (m, 1H) 1446 N-[4-(4-{[(2R)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.53- (ESI(+)) tetrahydrofuran-2- 8.44 (m, 1H), 8.41 (d, J = 6.7 Hz, 1H), 7.65-7.56 (m, m/e 433 ylcarbonyl]amino}cyclohex- 1H), 7.56-7.47 (m, 2H), 7.46-7.39 (m, 1H), 7.33 (d, (M + H)⁺ 1-en-1- J = 8.7 Hz, 2H), 6.01 (t, J = 4.3 Hz, 1H), 4.80 (d, J = yl)phenyl]-1,3-dihydro- 4.0 Hz, 4H), 4.24-4.16 (m, 1H), 3.93-3.82 (m, 3H), 2H-pyrrolo[3,4- 3.80-3.70 (m, 1H), 2.33 (dd, J = 5.3, 3.1 Hz, 1H), c]pyridine-2- 2.24-2.01 (m, 3H), 2.01-1.63 (m, 5H) carboxamide 1447 N-[4-(4-{[(1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.68-8.56 (m, 1H), (ESI(+)) methylpiperidin-4- 8.50 (d, J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.70 (d, J = 7.6 m/e 460 yl)carbonyl]amino}cyclohex- Hz, 1H), 7.56-7.48 (m, 2H), 7.43 (d, J = 5.2 Hz, 1H), (M + H)⁺ 1-en-1-yl)phenyl]-1,3-dihydro- 7.37-7.29 (m, 2H), 6.02 (bs, 1H), 4.83-4.77 (m, 2H-pyrrolo[3,4- 4H), 3.86-3.76 (m, 1H), 2.81-2.70 (m, 3H), 2.38- c]pyridine-2- 2.25 (m, 1H), 2.13 (s, 3H), 2.10-1.97 (m, 2H), 1.90- carboxamide 1.74 (m, 3H), 1.68-1.49 (m, 5H) 1448 N-[4-(4-{[(1,1- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) dioxidotetrahydro-2H- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.92 (d, J = 7.5 Hz, 1H), m/e 495 thiopyran-4- 7.56-7.49 (m, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.37- (M + H)⁺ yl)carbonyl]amino}cyclohex- 7.29 (m, 2H), 6.02 (bs, 1H), 4.87-4.77 (m, 4H), 3.83 1-en-1- (d, J = 3.0 Hz, 1H), 3.16-3.01 (m, 4H), 2.42 (d, J = yl)phenyl]-1,3-dihydro- 24.4 Hz, 4H), 2.11-1.91 (m, 5H), 1.93-1.78 (m, 2H-pyrrolo[3,4- 1H), 1.72-1.52 (m, 1H) c]pyridine-2- carboxamide 1449 N-[4-(4-{[(3R)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) tetrahydrofuran-3- J = 5.0 Hz, 1H), 8.42 (s, 1H), 7.92 (d, J = 7.5 Hz, 1H), m/e 433 ylcarbonyl]amino}cyclohex- 7.56-7.49 (m, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.37- (M + H)⁺ 1-en-1- 7.29 (m, 2H), 6.02 (bs, 1H), 4.88-4.72 (m, 4H), 3.84 yl)phenyl]-1,3-dihydro- (td, J = 8.1, 3.8 Hz, 2H), 3.76-3.55 (m, 3H), 2.93 (p, 2H-pyrrolo[3,4- J = 7.6 Hz, 1H), 2.42 (d, J = 19.4 Hz, 3H), 2.12-1.84 c]pyridine-2- (m, 4H), 1.69-1.51 (m, 1H) carboxamide 1450 N-[4-(4-{[(3S)- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, (ESI(+)) tetrahydrofuran-3- J = 5.0 Hz, 1H), 8.41 (s, 1H), 7.91 (d, J = 7.6 Hz, 1H), m/e 433 ylcarbonyl]amino}cyclohex- 7.54 (s, 2H), 7.43 (d, J = 5.1 Hz, 1H), 7.37-7.29 (m, (M + H)⁺ 1-en-1- 2H), 6.02 (bs, 1H), 4.85-4.72 (m, 4H), 3.84 (td, J = yl)phenyl]-1,3-dihydro- 8.1, 3.8 Hz, 2H), 3.78-3.55 (m, 3H), 2.93 (p, J = 7.7 2H-pyrrolo[3,4- Hz, 1H), 2.43 (d, J = 18.2 Hz, 2H), 2.11-1.79 (m, c]pyridine-2- 4H), 1.60 (s, 1H) carboxamide 1451 N-[4-(4-{[(2S)-2- ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.53- (ESI(+)) methylbutanoyl]amino} 8.43 (m, 1H), 8.42 (d, J = 6.6 Hz, 1H), 7.76-7.62 (m, m/e 419 cyclohex-1-en-1- 1H), 7.56-7.46 (m, 2H), 7.49-7.36 (m, 1H), 7.35- (M + H)⁺ yl)phenyl]-1,3-dihydro- 7.28 (m, 2H), 6.05-5.94 (m, 1H), 4.91-4.65 (m, 2H-pyrrolo[3,4- 4H), 4.06-3.70 (m, 1H), 2.48-2.31 (m, 2H), 2.24- c]pyridine-2- 1.98 (m, 2H), 1.94-1.77 (m, 1H), 1.70-1.40 (m, carboxamide 2H), 1.39-1.14 (m, 2H), 1.04-0.86 (m, 3H), 0.82 (td, J = 7.4, 3.3 Hz, 3H)

Example 1020 tert-butyl 3-{[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]methyl}azetidine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 3-(aminomethyl)azetidine-1-carboxylate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 7.37-7.23 (m, 4H), 6.58-6.48 (m, 1H), 4.58 (s, 4H), 3.91-3.75 (m, 2H), 3.65-3.51 (m, 2H), 3.30-3.20 (m, 2H), 2.68-2.55 (m, 1H), 1.35 (s, 9H); MS (ESI(+)) m/e 332 (M+H)⁺.

Example 1021 tert-butyl[(1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}azetidin-3-yl)methyl]carbamate Example 1021A tert-butyl (1-(4-nitrophenyl)azetidin-3-yl)methylcarbamate

A solution of 1-fluoro-4-nitrobenzene (0.61 g, 4.32 mmol) and tert-butyl azetidin-3-ylmethylcarbamate (0.886 g, 4.76 mmol) in dimethylformamide (8.65 ml) was treated with potassium carbonate (0.896 g, 6.48 mmol) and the suspension was heated at 55° C. (12 pm) for 3 hours and at ambient temperature for 16 hours. The reaction was poured into water and the suspension was filtered. The solid was washed with water and dried to provide the title compound.

Example 1021B tert-butyl (1-(4-aminophenyl)azetidin-3-yl)methylcarbamate

The title compound was prepared as described in Example 272A, substituting tert-butyl (1-(4-nitrophenyl)azetidin-3-yl)methylcarbamate for 4-nitro-N-propylbenzamide.

Example 1021C tert-butyl[(1-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}azetidin-3-yl)methyl]carbamate

The title compound was prepared as described in Example 272B, substituting tert-butyl (1-(4-aminophenyl)azetidin-3-yl)methylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.03 (s, 1H), 7.39-7.25 (m, 6H), 7.07-6.94 (m, 1H), 6.33 (d, J=8.8 Hz, 2H), 4.72 (s, 4H), 3.75 (t, J=7.4 Hz, 2H), 3.48-3.40 (m, 2H), 3.22-3.14 (m, 2H), 2.76-2.65 (m, 1H), 1.38 (s, 9H); MS (ESI(+)) m/e 423 (M+H)⁺.

Example 1046 N-[4-({[4-(acetylamino)phenyl]sulfonyl}amino)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and 4-(acetylamino)phenyl]sulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.72 (s, 1H) 8.62 (d, J=4.88 Hz, 1H) 7.73 (d, J=5.49 Hz, 1H) 7.61-7.69 (m, 4H) 7.36 (d, J=8.54 Hz, 2H) 6.98 (d, J=8.85 Hz, 2H) 4.88 (d, J=7.02 Hz, 4H) 2.00-2.10 (m, 3H); MS (APCI(+)) m/e 452 (M+H)⁺.

Example 1047 N-{4-[(propylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and propylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.72 (s, 1H) 8.62 (d, J=5.49 Hz, 1H) 7.73 (d, J=5.49 Hz, 1H) 7.46 (d, J=8.54 Hz, 2H) 7.14 (d, J=8.85 Hz, 2H) 4.91 (d, J=6.10 Hz, 4H) 2.98-3.06 (m, 2H) 1.66-1.78 (m, 2H) 0.96 (t, J=7.48 Hz, 3H); MS (APCI(+)) m/e 361 (M+H)⁺.

Example 1048 N-(4-{[(4-propylphenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and (4-propylphenyl)sulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (300 MHz, DMSO-d₆) δ 9.90 (s, 1H), 8.59 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.33 (s, 1H), 7.64-7.58 (m, 2H), 7.45-7.33 (m, 4H), 7.33 (s, 1H), 6.99-6.92 (m, 2H), 4.79-4.72 (m, 4H), 2.57 (dd, J=17.1, 9.3 Hz, 1H), 1.65-1.49 (m, 2H), 0.86 (t, J=7.3 Hz, 3H); MS (ESI(+)) m/e 437 (M+H)⁺.

Example 1049 N-{4-[(butylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and butylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.71 (s, 1H) 8.61 (d, J=5.19 Hz, 1H) 7.70 (d, J=5.49 Hz, 1H) 7.47 (d, J=8.85 Hz, 2H) 7.14 (d, J=8.85 Hz, 2H) 4.90 (d, J=3.66 Hz, 4H) 2.97-3.08 (m, 2H) 1.61-1.72 (m, 2H) 1.30-1.44 (m, 2H) 0.85 (t, J=7.32 Hz, 3H); MS (APCI(+)) m/e 375 (M+H)⁺.

Example 1050 N-{4-[({[(1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methyl}sulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and (1S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methyl}sulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) δ ppm 8.72 (s, 1H) 8.61 (d, J=5.19 Hz, 1H) 7.71 (d, J=5.49 Hz, 1H) 7.49 (d, J=8.85 Hz, 2H) 7.18 (d, J=8.85 Hz, 2H) 4.90 (d, J=3.97 Hz, 4H) 2.81 (s, 2H) 2.27-2.41 (m, 2H) 2.07 (t, J=4.43 Hz, 1H) 1.94-2.03 (m, 2H) 1.34-1.66 (m, 2H) 1.02 (s, 3H) 0.79 (s, 3H); MS (APCI(+)) m/e 469 (M+H)⁺.

Example 1051 N-{4-[(ethylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and ethylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.70-8.75 (m, 1H) 8.60-8.64 (m, J=5.65, 5.65 Hz, 1H) 7.74 (d, J=5.19 Hz, 1H) 7.46 (d, J=8.85 Hz, 2H) 7.15 (d, J=8.54 Hz, 2H) 4.91 (d, J=7.02 Hz, 4H) 3.04 (q, J=7.32 Hz, 2H) 1.23 (t, J=7.32 Hz, 3H); MS (APCI(+)) m/e 347 (M+H)⁺.

Example 1052 N-{4-[(benzylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and benzylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.72 (s, 1H) 8.61 (d, J=4.88 Hz, 1H) 7.70 (d, J=5.19 Hz, 1H) 7.46 (d, J=8.85 Hz, 2H) 7.28-7.37 (m, 5H) 7.11 (d, J=8.85 Hz, 2H) 4.90 (d, J=3.05 Hz, 4H) 4.37 (s, 2H); MS (APCI(+)) m/e 409 (M+H)⁺.

Example 1053 N-(4-{[(4-fluorophenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and (4-fluorophenyl)sulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.71 (s, 1H) 8.61 (d, J=5.19 Hz, 1H) 7.78 (dd, J=8.85, 5.19 Hz, 2H) 7.67-7.73 (m, 1H) 7.28-7.43 (m, 4H) 6.98 (d, J=8.85 Hz, 2H) 4.87 (d, J=4.27 Hz, 4H); MS (APCI(+)) m/e 412 (M+H)⁺.

Example 1054 N-{4-[(thiophen-2-ylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and thiophen-2-ylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.70 (s, 1H) 8.61 (d, J=4.88 Hz, 1H) 7.81 (d, J=4.88 Hz, 1H) 7.69 (d, J=5.19 Hz, 1H) 7.49 (d, J=2.75 Hz, 1H) 7.42 (d, J=8.85 Hz, 2H) 7.09-7.13 (m, 1H) 7.04 (d, J=8.85 Hz, 2H) 4.88 (d, J=3.36 Hz, 4H); MS (APCI(+)) m/e 401 (M+H)⁺.

Example 1088 N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 4-(piperidin-1-ylsulfonyl)aniline for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.89 (s, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 7.86-7.79 (m, 2H), 7.66-7.59 (m, 2H), 7.44 (d, J=5.0 Hz, 1H), 4.89-4.76 (m, 4H), 3.25-3.00 (m, 1H), 2.95-2.82 (m, 4H), 1.57-1.44 (m, 4H), 1.41-1.31 (m, 1H); MS (ESI(+)) m/e 387 (M+H)⁺.

Example 1246 methyl 1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate Example 1246A methyl 1-(4-nitrophenyl)azetidine-3-carboxylate

A solution of methyl azetidine-3-carboxylate hydrochloride (1.236 g, 8.15 mmol) and N-methylmorpholine (2.338 ml, 21.26 mmol) in dimethylformamide (10 mL) was treated with a solution of 1-fluoro-4-nitrobenzene (1 g, 7.09 mmol) in dimethylformamide (7 mL) and the reaction was allowed to stir at room temperature for 60 hours. Water (50 mL) was added and the resulting suspension was stirred 10 minutes and filtered. The collected solid was washed with water and dried under vacuum. Flash chromatography of the collected solid provided the title compound.

Example 1246B methyl 1-(4-aminophenyl)azetidine-3-carboxylate

The title compound was prepared as described in Example 272A, substituting methyl 1-(4-nitrophenyl)azetidine-3-carboxylate for 4-nitro-N-propylbenzamide.

Example 1246C methyl 1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate

The title compound was prepared as described in Example 272B, substituting methyl 1-(4-aminophenyl)azetidine-3-carboxylate for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.15 (s, 1H), 7.42 (d, J=5.1 Hz, 1H), 7.36-7.29 (m, 2H), 6.44-6.37 (m, 2H), 4.80-4.72 (m, 4H), 4.02-3.93 (m, 2H), 3.86-3.77 (m, 2H), 3.68 (s, 3H), 3.66-3.56 (m, 1H); MS (ESI(+)) m/e 353 (M+H)⁺.

Example 1247 N-(4-{3-[(3-methylbutyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1247A 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid

The title compound was prepared as described in Example 1B, substituting methyl 1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 1247B N-(4-{3-[(3-methylbutyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-methylbutan-1-amine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.13 (s, 1H), 7.90 (t, J=5.5 Hz, 1H), 7.42 (d, J=4.8 Hz, 1H), 7.34-7.27 (m, 2H), 6.41-6.34 (m, 2H), 4.79-4.73 (m, 4H), 3.94-3.85 (m, 2H), 3.76-3.69 (m, 2H), 3.47-3.36 (m, 1H), 3.13-3.04 (m, 2H), 1.65-1.48 (m, 1H), 1.35-1.24 (m, 2H), 0.87 (d, J=6.6 Hz, 6H); MS (ESI(+)) m/e 408 (M+H)⁺.

Example 1248 N-(4-{3-[(tetrahydrofuran-2-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (tetrahydrofuran-2-yl)methanamine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.13 (s, 1H), 8.05 (t, J=5.8 Hz, 1H), 7.42 (d, J=5.1 Hz, 1H), 7.35-7.27 (m, 2H), 6.41-6.34 (m, 2H), 4.79-4.73 (m, 4H), 3.94-3.68 (m, 6H), 3.68-3.55 (m, 1H), 3.54-3.39 (m, 1H), 3.20-3.07 (m, 2H), 1.93-1.71 (m, 3H), 1.55-1.41 (m, 1H); MS (ESI(+)) m/e 422 (M+H)⁺.

Example 1249 N-(4-{3-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (tetrahydro-2H-pyran-4-yl)methanamine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.13 (s, 1H), 7.97 (t, J=5.8 Hz, 1H), 7.42 (d, J=5.1 Hz, 1H), 7.34-7.27 (m, 2H), 6.41-6.34 (m, 2H), 4.79-4.73 (m, 4H), 3.95-3.86 (m, 2H), 3.86-3.78 (m, 2H), 3.77-3.69 (m, 2H), 3.51-3.40 (m, 1H), 3.31-3.19 (m, 2H), 3.02-2.94 (m, 2H), 1.69-1.48 (m, 3H), 1.22-1.04 (m, 2H); MS (ESI(+)) m/e 436 (M+H)⁺.

Example 1250 N-{4-[3-(benzylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting benzylamine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.53-8.45 (m, 2H), 8.13 (s, 1H), 7.42 (d, J=5.0 Hz, 1H), 7.37-7.22 (m, 7H), 6.43-6.35 (m, 2H), 4.76 (m, 4H), 4.30 (d, J=5.9 Hz, 2H), 3.99-3.88 (m, 2H), 3.83-3.72 (m, 2H), 3.57-3.46 (m, 1H); MS (ESI(+)) m/e 428 (M+H)⁺.

Example 1251 N-{4-[3-(cyclopentylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting cyclopentylamine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.13 (s, 1H), 7.91 (d, J=7.2 Hz, 1H), 7.42 (d, J=5.1 Hz, 1H), 7.34-7.27 (m, 2H), 6.41-6.33 (m, 2H), 4.79-4.73 (m, 4H), 4.06-3.94 (m, 1H), 3.92-3.84 (m, 2H), 3.76-3.66 (m, 2H), 3.46-3.33 (m, 1H), 1.86-1.72 (m, 2H), 1.67-1.30 (m, 6H); MS (ESI(+)) m/e 406 (M+H)⁺.

Example 1252 N-(4-{3-[(cyclopentylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting cyclopentylmethamine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.13 (s, 1H), 7.96 (t, J=5.7 Hz, 1H), 7.42 (d, J=4.7 Hz, 1H), 7.34-7.27 (m, 2H), 6.41-6.33 (m, 2H), 4.81-4.72 (m, 4H), 3.94-3.85 (m, 2H), 3.77-3.68 (m, 2H), 3.50-3.37 (m, 1H), 3.04-2.97 (m, 2H), 2.04-1.89 (m, 1H), 1.71-1.39 (m, 6H), 1.25-1.08 (m, 2H); MS (ESI(+)) m/e 420 (M+H)⁺.

Example 1253 N-(4-{3-[(2-methoxyethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 2-methoxyeth-1-ylamine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)azetidine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.13 (s, 1H), 8.05 (t, J=5.5 Hz, 1H), 7.42 (d, J=5.1 Hz, 1H), 7.35-7.27 (m, 2H), 6.42-6.34 (m, 2H), 4.79-4.73 (m, 4H), 3.93-3.86 (m, 2H), 3.73 (t, J=6.6 Hz, 2H), 3.52-3.41 (m, 1H), 3.38-3.30 (m, 2H), 3.27-3.21 (m, 5H); MS (ESI(+)) m/e 396 (M+H)⁺.

Example 1268 N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (5)-(tetrahydrofuran-2-yl)methamine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.03 (s, 1H), 8.85 (t, J=6.1 Hz, 1H), 8.32 (d, J=9.3 Hz, 1H), 8.12 (d, J=9.3 Hz, 1H), 7.41-7.28 (m, 4H), 5.04-4.72 (m, 4H), 4.04 (p, J=6.2 Hz, 1H), 3.85-3.74 (m, 1H), 3.69-3.58 (m, 1H), 3.38 (dd, J=11.2, 5.0 Hz, 2H), 2.01-1.74 (m, 3H), 1.71-1.54 (m, 1H); MS (ESI(+)) m/e 368 (M+H)⁺.

Example 1285 N-{4-[(4-fluorobenzyl)(3-methylbutanoyl)amino]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide Example 1285A tert-butyl 4-(4-fluorobenzylamino)butylcarbamate

Tert-butyl 4-bromobutylcarbamate (0.735 g, 2.91 mmoles), (4-fluorophenyl)methanamine (0.333 g, 2.91 mmoles) and potassium carbonate (0.806 g, 5.83 mmoles) were stirred in acetonitrile (15 mL) at 100° C. for 1 hour. The reaction mixture was cooled, the solvent wags concentrated and the residue was taken into dichloromethane and washed with water twice. The organic layers were combined, dried over magnesium sulfate, filtered and concentrated to provide the title compound which was used without further purification in the next step.

Example 1285B tert-butyl 4-(N-(4-fluorobenzyl)-3-methylbutanamido)butylcarbamate

The title compound was prepared as described in Example 278, substituting 3-methylbutanoyl chloride for acetyl chloride and tert-butyl 4-(4-fluorobenzylamino)butylcarbamate for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide.

Example 1285C N-(4-aminobutyl)-N-(4-fluorobenzyl)-3-methylbutanamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(N-(4-fluorobenzyl)-3-methylbutanamido)butylcarbamate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1285D N-{4-[(4-fluorobenzyl)(3-methylbutanoyl)amino]butyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 272B, substituting N-(4-aminobutyl)-N-(4-fluorobenzyl)-3-methylbutanamide for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (400 MHz, CDCl₃) δ ppm 7.34-7.27 (m, 4H), 7.23 (dd, J=8.5, 5.5 Hz, 1H), 7.13 (dd, J=8.5, 5.5 Hz, 1H), 7.06 (t, J=8.6 Hz, 1H), 6.99 (t, J=8.6 Hz, 1H), 5.49-5.17 (m, 1H), 4.72 (m, 4H), 4.56 (d, J=17.7 Hz, 2H), 3.34 (m, 4H), 2.29 (m, 2H), 2.23-2.12 (m, 1H), 1.68-1.50 (m, 4H), 1.01-0.93 (d, J=6.9 Hz, 6H); MS (APCI(+)) m/e 426 (M+H)⁺.

Example 1286 N-[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1286A 4-(but-3-enyloxy)-6-chloroquinolin-2(1H)-one

To a solution of 6-chloro-4-hydroxyquinolin-2(1H)-one (800 mg, 4.09 mmol) and N,N-diisopropylethylamine (1415 μl, 8.18 mmol) in dimethylformamide (13.6 ml) was added 4-bromo-1-butene (415 μl, 4.09 mmol). The solution was heated to 60° C. and stirred for 18 hours. The reaction mixture was purified by column chromatography to provide the title compound.

Example 1286B 9-chloro-3,3a,4,4a-tetrahydro-2H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-5(6H)-one

A solution of 4-(but-3-enyloxy)-6-chloroquinolin-2(1H)-one (600 mg, 2.403 mmol) in benzene (240 mL) was placed under a 450 W Hg UV lamp (fitted with a condenser for cooling) and stirred for 4 days (96 hours). The mixture was then cooled, concentrated in vacuo, and taken up in 75 mL of methylene chloride (with mild heating to dissolve as much as possible). The sample, which was a mixture of regioisomers, was purified by column chromatography. Concentration of the compound that eluted second provided the title compound.

Example 1286C tert-butyl[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]carbamate

To a solution of 9-chloro-3,3a,4,4a-tetrahydro-2H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-5(6H)-one (200 mg, 0.801 mmol) in dimethylformamide (4 ml) at 0° C. was slowly added sodium hydride (19 mg, 0.801 mmol) over 15 minutes. The suspension was allowed to warm to room temperature. The mixture stirred for 45 minutes and 4-(Boc-amino)butyl bromide (202 mg, 0.801 mmol) was added. The solution was stirred for 15 hours, followed by addition of 0.25 mL methanol. Column chromatography provided the title compound.

Example 1286D 6-(4-aminobutyl)-9-chloro-3,3a,4,4a-tetrahydro-2H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-5(6H)-one

The title compound was prepared as described in Example 2D, substituting tert-butyl[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]carbamate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1286E N-[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 272B, substituting 6-(4-aminobutyl)-9-chloro-3,3a,4,4a-tetrahydro-2H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-5(6H)-one for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (400 MHz, CDCl₃) δ ppm 8.58 (s, 1H), 8.54 (d, J=4.9 Hz, 1H), 7.29 (d, J=4.9 Hz, 1H), 7.25 (m, 1H), 7.23 (d, J=2.6 Hz, 1H), 6.92 (d, J=8.9 Hz, 1H), 4.84 (t, J=5.6 Hz, 1H), 4.74 (bs, 4H), 4.46 (t, J=8.1 Hz, 1H), 4.22 (m, 1H), 4.05 (m, 1H), 3.91 (m, 1H), 3.39 (m, 3H), 2.93 (m, 1H), 2.31 (m, 1H), 2.22 (m, 1H), 1.84 (m, 1H), 1.69 (m, 5H); MS (ESI(+)) m/e 467 (M+H)⁺.

Example 1287 N-{4-[7-chloro-1-(2-hydroxyethyl)-3-oxo-1,3-dihydrocyclobuta[c]quinolin-4(2H)-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

To a solution of N-[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide (30 mg, 0.064 mmol) in dimethylformamide (292 uL) and water (292 uL) was added sodium hydroxide (1.679 μl, 0.064 mmol). The solution was stirred for 18 hours and then brought to pH ˜7 by dropwise addition of 1M HCl. Column chromatography of the wet, crude mixture provided the title compound. ¹H NMR (400 MHz, CDCl₃) δ ppm 8.58 (s, 1H), 8.54 (d, J=5.1 Hz, 1H), 7.54 (d, J=2.4 Hz, 1H), 7.46 (dd, J=9.1, 2.4 Hz, 1H), 7.37 (d, J=9.1 Hz, 1H), 7.25 (m, 1H), 5.06 (t, J=5.7 Hz, 1H) 4.77 (bs, 2H), 4.75 (bs, 2H), 4.33 (t, J=7.4 Hz, 2H), 3.87 (m, 2H), 3.74 (m, 2H), 3.46 (m, 2H), 3.37 (dd, J=14.0, 4.5 Hz, 1H), 2.86 (dd, J=14.0, 1.3 Hz, 1H), 2.27 (m, 1H), 1.97 (m, 1H), 1.82 (m, 2H), 1.71 (m, 2H); MS (ESI(+)) m/e 467 (M+H)⁺.

Example 1290 N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (R)-(tetrahydrofuran-2-yl)methamine for 3-phenylpropan-1-amine and 6-(isoindoline-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.02 (s, 1H), 8.85 (t, J=6.1 Hz, 1H), 8.32 (d, J=9.3 Hz, 1H), 8.12 (d, J=9.3 Hz, 1H), 7.41-7.28 (m, 4H), 5.00-4.71 (m, 4H), 4.04 (p, J=6.2 Hz, 1H), 3.85-3.74 (m, 1H), 3.70-3.58 (m, 1H), 3.44-3.33 (m, 3H), 1.99-1.71 (m, 2H), 1.69-1.54 (m, 1H); MS (ESI(+)) m/e 368 (M+H)⁺.

TABLE 21 The following Examples were essentially prepared as described in Example 1C, substituting N-(4-aminophenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1- amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 1363 N-{4-[(3- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.71 (APCI(+)) ethoxypropanoyl)amino]phenyl}- (s, 1H), 8.61 (d, J = 5.4 Hz, 1H), 7.70 (d, J = 5.5 m/e 355 1,3-dihydro-2H- Hz, 1H), 7.44 (m, 4H), 4.89 (m, 4H), 3.68 (t, J = (M + H)⁺ pyrrolo[3,4-c]pyridine-2- 4.7 Hz, 2H), 3.47 (q, J = 7.0 Hz, 2H), 2.52 (m, carboxamide 2H), 1.11 (t, J = 7.0 Hz, 3H) 1364 N-(4-{[(1-acetylpiperidin-4- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.73 (APCI (+)) yl)carbonyl]amino}phenyl)- (s, 1H), 8.62 (d, J = 5.46, 1H), 7.75 (m, 1H), 7.41 m/e 408 1,3-dihydro-2H- (m, 4H), 4.91 (m, 4H), 4.13 (m, 2H), 2.95 (m, (M + H)⁺ pyrrolo[3,4-c]pyridine-2- 2H), 2.60 (m, 1H), 1.99 (m, 3H), 1.84 (m, 2H), carboxamide 1.52 (m, 2H) 1365 N-{4- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.69 (APCI (+)) [(ethoxyacetyl)amino]phenyl}- (s, 1H), 8.59(d, J = 5.4 Hz, 1H), 7.66 (d, J = 5.5 m/e 341 1,3-dihydro-2H- Hz, 1H), 7.48 (m, 4H), 4.89 (bs, 4H), 4.00 (s, (M + H)⁺ pyrrolo[3,4-c]pyridine-2- 2H), 3.60(q, J = 7.0 Hz, 2H), 1.21 (t, J = 6.9 Hz, carboxamide 3H) 1366 N-{4-[(tetrahydrofuran-2- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.70 (APCI (+)) ylcarbonyl)amino]phenyl}- (s, 1H), 8.60 (d, J = 5.4 Hz, 1H), 7.69 (d, J = 5.5 m/e 353 1,3-dihydro-2H- Hz, 1H), 7.48 (m, 4H), 4.89 (m, 4H), 4.35 (dd, J = (M + H)⁺ pyrrolo[3,4-c]pyridine-2- 8.1, 5.6 Hz, 1H), 4.00 (m, 1H), 3.83 (dt, J = carboxamide 8.1, 6.7 Hz, 1H), 2.92 (m, 1H), 2.71 (s, 1H), 2.23 (m, 1H), 2.00 (m, 1H), 1.92 (m, 2H) 1367 N-{4-[(tetrahydrofuran-3- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.73 (APCI (+)) ylcarbonyl)amino]phenyl}- (m, 1H), 8.61 (m, 1H), 7.70 (m, 1H), 7.43 (m, m/e 353 1,3-dihydro-2H- 4H), 4.90 (d, J = 8.2 Hz, 4H), 3.93 (m, 1H), 3.76 (M + H)⁺ pyrrolo[3,4-c]pyridine-2- (m, 3H), 3.13 (m, 1H), 2.10 (q, J = 7.2 Hz, 2H) carboxamide 1368 N-{4- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.67 (APCI (+)) [(cyclopentylcarbonyl)ami- (s, 1H), 8.57 (d, J = 5.3 Hz, 1H), 7.62 (d, J = 5.4 m/e 351 no]phenyl}-1,3-dihydro-2H- Hz, 1H), 7.44 (m, 4H), 4.87 (s, 4H), 2.77 (m, (M + H)⁺ pyrrolo[3,4-c]pyridine-2- 1H), 1.70 (m, 8H) carboxamide 1370 N-{4-[(bicyclo[2.2.1]hept- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.66 (APCI (+)) 2-ylacetyl)amino]phenyl}- (s, 1H), 8.56 (d, J = 5.3 Hz, 1H), 7.60 (d, J = 5.2 m/e 391 1,3-dihydro-2H- Hz, 1H), 7.43 (m, 4H), 4.86 (s, 4H), 2.25 (dd, J = (M + H)⁺ pyrrolo[3,4-c]pyridine-2- 14.1, 7.8 Hz, 1H), 2.20 (s, 1H), 2.12 (dd, J = carboxamide 14.0, 7.6 Hz, 1H), 1.98 (d, J = 17.2 Hz, 1H), 1.90 (s, 1H), 1.41 (m, 4H), 1.14 (m, 4H) 1371 N-{4-[(1,3-thiazol-5- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 9.20 (APCI (+)) ylcarbonyl)amino]phenyl}- (s, 1H), 8.67 (s, 1H), 8.60 (s, 1H), 8.57 (d, J = 5.3 m/e 366 1,3-dihydro-2H- Hz, 1H), 7.61 (d, J = 5.3 Hz, 4H), 7.55 (m, 4H) (M + H)⁺ pyrrolo[3,4-c]pyridine-2- carboxamide 1372 N-(4-{[(4-oxo-4,5,6,7- ¹H NMR (400 MHz, DMSO/D₂O, 90° C.) δ 8.65 (APCI (+)) tetrahydro-1-benzofuran-3- (s, 1H), 8.55 (d, J = 5.2 Hz, 1H), 8.26 (d, J = 14.4 m/e 417 yl)carbonyl]amino}phenyl)- Hz, 1H), 7.55 (m, 5H), 4.86 (s, 4H), 2.96 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 2.64 (m, 2H), 2.18 (m, 2H) pyrrolo[3,4-c]pyridine-2- carboxamide

Example 1369 N-{7-oxo-7-[(3-phenylpropyl)amino]heptyl}-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 7-(isoindoline-2-carboxamido)heptanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid.

Example 1373 N-(4-{2-[(3-methylbutanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 1373A N-(4-(2-aminoethyl)phenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl (2-{4-[(1,3-dihydro-2H-isoindol-2-ylcarbonyl)amino]phenyl}ethyl)carbamate for tert-butyl 4-44-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1373B N-(4-{2-[(3-methylbutanoyl)amino]ethyl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(2-aminoethyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 3-methylbutanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆, Temp=90° C.) δ 7.50-7.40 (m, 2H), 7.40-7.24 (m, 4H), 7.13-7.02 (m, 2H), 4.76 (s, 4H), 2.68 (t, J=7.3 Hz, 2H), 2.07-1.84 (m, 3H), 0.95-0.76 (m, 6H). MS (ESI (+)) m/e 366 (M+H)⁺.

TABLE 22 The following Examples were essentially prepared as described in Example 1C, substituting N-(4-(2-aminoethyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and the appropriate carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 1374 N-(4-{2-[(4- ¹H NMR (400 MHz, DMSO-_(6,) Temp = 90° C.) δ (ESI(+)) methylpentanoyl)amino]eth- 7.44 (t, J = 8.2 Hz, 2H), 7.38-7.18 (m, 4H), 7.18- m/e 380 yl}phenyl)-1,3-dihydro- 6.99 (m, 2H), 4.76 (s, 4H), 2.78-2.60 (m, 2H), (M + H)⁺ 2H-isoindole-2- 2.13-1.99 (m, 2H), 1.58-1.33 (m, 3H), 0.90- carboxamide 0.79 (m, 6H) 1375 N-(4-{2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(ethoxyacetyl)amino]eth- 8.07-7.98 (m, 1H), 7.50-7.25 (m, 7H), 7.11 (t, m/e 368 yl]phenyl)-1,3-dihydro-2H- J = 6.6 Hz, 2H), 4.76 (s, 4H), 3.80 (s, 2H), 3.55- (M + H)⁺ isoindole-2-carboxamide 3.41 (m, 2H), 3.41-3.33 (m, 2H), 2.78-2.64 (m, 2H), 1.19-1.07 (m, 3H) 1376 N-[4-(2-{[(2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) methoxyethoxy)acetyl]ami- 7.45 (d, J = 8.4 Hz, 2H), 7.40-7.25 (m, 4H), 7.20- m/e 398 no}ethyl)phenyl]-1,3- 6.98 (m, 2H), 4.76 (s, 4H), 3.85 (s, 2H), 3.67- (M + H)⁺ dihydro-2H-isoindole-2- 3.51 (m, 2H), 3.51-3.42 (m, 2H), 3.41-3.33 (m, carboxamide 2H), 3.28 (s, 5H), 2.76-2.64 (m, 2H) 1377 N-(4-{2-[(tetrahydrofuran-2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) ylcarbonyl)amino]ethyl}phenyl)- 7.52-7.37 (m, 2H), 7.37-7.21 (m, 4H), 7.10 (t, m/e 380 1,3-dihydro-2H- J = 7.3 Hz, 2H), 4.76 (s, 4H), 4.28-4.03 (m, 1H), (M + H)⁺ isoindole-2-carboxamide 3.89-3.78 (m, 1H), 3.80-3.65 (m, 1H), 3.53- 3.31 (m, 2H), 2.75-2.60 (m, 2H), 2.20-2.02 (m, 1H), 1.94-1.64 (m, 3H) 1378 N-(4-{2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(cyclopentylcarbonyl)ami- 7.43 (d, J = 8.5 Hz, 2H), 7.37-7.21 (m, 4H), 7.09 m/e 378 no]ethyl}phenyl)-1,3- (d, J = 8.4 Hz, 2H), 4.76 (s, 4H), 2.68 (t, J = 7.3 (M + H)⁺ dihydro-2H-isoindole-2- Hz, 2H), 1.61 (t, J = 44.5 Hz, 8H) carboxamide 1379 N-(4-{2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) [(cyclopentylacetyl)amino] 7.43 (dd, J = 6.3, 4.5 Hz, 2H), 7.37-7.24 (m, m/e 392 ethyl}phenyl)-1,3-dihydro- 4H), 7.09 (d, J = 8.4 Hz, 2H), 4.76 (s, 4H), 2.67 (M + H)⁺ 2H-isoindole-2- (dd, J = 9.4, 5.3 Hz, 2H), 2.23-1.94 (m, 4H), carboxamide 1.76-1.42 (m, 6H), 1.22-1.05 (m, 2H) 1380 N-{4-[2- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) (benzoylamino)ethyl]phenyl}- 7.82-7.73 (m, 2H), 7.56-7.40 (m, 5H), 7.37- m/e 386 1,3-dihydro-2H- 7.25 (m, 4H), 7.20-7.07 (m, 2H), 4.76 (s, 4H), (M + H)⁺ isoindole-2-carboxamide 3.51 (t, J = 7.4 Hz, 2H), 2.93-2.67 (m, 2H) 1381 N-(4-{2-[(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-4- 7.49-7.38 (m, 2H), 7.37-7.24 (m, 4H), 7.09 (d, m/e 394 ylcarbonyl)amino]ethyl}phenyl)- J = 8.4 Hz, 2H), 4.76 (s, 4H), 3.90-3.74 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 3.37-3.30 (m, 2H), 2.68 (t, J = 7.3 Hz, 2H), 2.39- isoindole-2-carboxamide 2.23 (m, 1H), 1.66-1.48 (m, 4H) 1382 N-(4-{2-[(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) pyran-4- 7.43 (t, J = 5.4 Hz, 2H), 7.40-7.24 (m, 4H), 7.09 m/e 408 ylacetyl)amino]ethyl}phenyl)- (d, J = 8.4 Hz, 2H), 4.76 (s, 4H), 3.85-3.68 (m, (M + H)⁺ 1,3-dihydro-2H- 2H), 3.28-3.24 (m, 4H), 2.68 (t, J = 7.3 Hz, 2H), isoindole-2-carboxamide 2.01 (d, J = 7.1 Hz, 2H), 1.94-1.76 (m, 1H), 1.59- 1.42 (m, 2H), 1.29-1.03 (m, 2H) 1383 N-(4-{2-[(tetrahydrofuran- ¹H NMR (400 MHz, DMSO-d_(6,) Temp = 90° C.) δ (ESI(+)) 3-ylacetyl)amino]ethyl}phenyl)- 7.53-7.35 (m, 3H), 7.42-7.22 (m, 4H), 7.09 (d, m/e 394 1,3-dihydro-2H- J = 8.4 Hz, 2H), 4.76 (s, 4H), 3.82-3.55 (m, 3H), (M + H)⁺ isoindole-2-carboxamide 3.35-3.30 (m, 1H), 3.26 (dd, J = 7.1, 5.3 Hz, 2H), 2.68 (t, J = 7.3 Hz, 2H), 2.48-2.36 (m, 1H), 2.22-2.07 (m, 2H), 2.04-1.81 (m, 1H), 1.62- 1.29 (m, 1H)

Example 1404 N-(4-{[1-(2-cyclopropylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting 2-cyclopropylacetaldehyde for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.54-8.58 (m, 2H) 8.08 (s, 1H) 7.72-7.77 (m, 2H) 7.10 (d, J=4.88 Hz, 1H) 7.01 (d, J=9.16 Hz, 2H) 4.82-4.88 (m, 4H) 3.71 (s, 1H) 2.74-2.82 (m, 2H) 2.43-2.50 (m, 2H) 2.22-2.31 (m, 2H) 1.97 (s, 2H) 1.79-1.90 (m, 2H) 1.35-1.47 (m, 2H) 0.70 (s, 1H) 0.36-0.45 (m, 2H) 0.05 (q, J=4.78 Hz, 2H); MS (APCI(+)) m/e 407 (M+H)⁺.

Example 1405 N-(4-{[1-(2-cyclopentylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting 2-cyclopentylacetaldehyde for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.54-8.58 (m, 2H) 8.08 (s, 1H) 7.72-7.78 (m, 2H) 7.10 (d, J=4.88 Hz, 1H) 7.00-7.04 (m, 2H) 4.82-4.90 (m, 4H) 4.21-4.31 (m, 1H) 2.73-2.83 (m, 2H) 2.34-2.40 (m, 2H) 2.20-2.29 (m, 2H) 1.96-2.03 (m, 2H) 1.67-1.93 (m, 5H) 1.40-1.62 (m, 6H) 1.04-1.17 (m, 2H); MS (APCI(+)) m/e 435 (M+H)⁺.

Example 1406 N-(4-{[1-(2-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting 2-methylbutanal for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.52-8.58 (m, 2H) 8.08 (s, 1H) 7.74 (d, J=8.85 Hz, 2H) 7.10 (d, J=4.58 Hz, 1H) 6.97-7.05 (m, 2H) 4.84 (d, J=6.71 Hz, 4H) 2.72 (d, J=10.68 Hz, 2H) 2.13-2.26 (m, 3H) 2.01-2.07 (m, 2H) 1.91-2.00 (m, 2H) 1.83 (s, 2H) 1.54 (s, 2H) 1.14 (s, 1H) 0.81-0.95 (m, 6H); MS (APCI(+)) m/e 409 (M+H)⁺.

Example 1407 N-(4-{[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting tetrahydrofuran-3-carbaldehyde for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.53-8.58 (m, 1H) 8.08 (s, 1H) 7.70-7.77 (m, 2H) 7.10 (d, J=5.19 Hz, 1H) 7.01 (d, J=8.85 Hz, 2H) 4.84 (d, J=7.63 Hz, 4H) 4.19-4.27 (m, 1H) 3.75-3.90 (m, 2H) 3.67-3.72 (m, 1H) 3.56 (dd, J=8.55, 5.80 Hz, 1H) 2.65-2.82 (m, 2H) 2.31-2.45 (m, 1H) 2.15-2.31 (m, 4H) 1.71-2.00 (m, 5H) 1.48-1.59 (m, 1H); MS (APCI(+)) m/e 423 (M+H)⁺.

Example 1408 N-(4-{[1-(3,3-dimethylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting 3,3-dimethylbutanal for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.52-8.58 (m, 2H) 8.09 (s, 1H) 7.71-7.78 (m, 2H) 7.10 (d, J=4.88 Hz, 1H) 6.99-7.04 (m, 2H) 4.84 (dd, J=8.39, 1.68 Hz, 4H) 3.85 (d, J=13.43 Hz, 1H) 2.75-2.85 (m, 2H) 2.38-2.47 (m, 2H) 2.21-2.34 (m, 2H) 1.98 (d, J=2.14 Hz, 2H) 1.78-1.91 (m, 2H) 1.39-1.49 (m, 2H) 0.84-0.92 (m, 9H); MS (APCI(+)) m/e 423 (M+H)⁺.

Example 1409 N-(4-{[1-(cyclohexylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting cyclohexanecarbaldehyde for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.53-8.57 (m, 2H) 8.08 (s, 1H) 7.69-7.77 (m, 2H) 7.10 (s, 1H) 6.97-7.04 (m, 2H) 4.82-4.87 (m, 4H) 4.20-4.27 (m, 1H) 2.73 (t, J=10.68 Hz, 2H) 2.17-2.26 (m, 2H) 2.13 (d, J=7.02 Hz, 2H) 1.93-2.01 (m, 2H) 1.76-1.87 (m, 4H) 1.55-1.72 (m, 3H) 1.44-1.54 (m, 1H) 1.09-1.29 (m, 3H) 0.89 (d, J=12.51 Hz, 2H); MS (APCI(+)) m/e 435 (M+H)⁺.

Example 1410 N-(4-{[1-(3-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting 3-methylbutanal for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.53-8.57 (m, 2H) 8.09 (s, 1H) 7.70-7.78 (m, 2H) 7.10 (d, J=5.19 Hz, 1H) 6.98-7.04 (m, 2H) 4.79-4.89 (m, 4H) 4.26 (d, J=3.66 Hz, 1H) 2.72-2.83 (m, 2H) 2.34-2.41 (m, 2H) 2.21-2.30 (m, 2H) 1.96-2.03 (m, 2H) 1.79-1.91 (m, 2H) 1.54-1.68 (m, 1H) 1.35-1.44 (m, 2H) 0.86-0.90 (m, 6H); MS (APCI(+)) m/e 408 (M+H)⁺.

Example 1411 N-(4-{[1-(cyclopentylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting cyclopentanecarbaldehyde for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.53-8.57 (m, 2H) 8.08 (s, 1H) 7.70-7.77 (m, 2H) 7.10 (d, J=4.88 Hz, 1H) 6.97-7.05 (m, 2H) 4.84 (dd, J=8.54, 1.53 Hz, 4H) 4.23-4.27 (m, 1H) 2.75 (d, J=10.99 Hz, 2H) 2.18-2.29 (m, 4H) 2.04 (s, 1H) 1.94-2.02 (m, 2H) 1.77-1.90 (m, 2H) 1.65-1.76 (m, 2H) 1.42-1.59 (m, 4H) 1.17-1.32 (m, 2H); MS (APCI(+)) m/e 420 (M+H)⁺.

Example 1412 N-(4-{[1-(tetrahydrofuran-2-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting tetrahydrofuran-2-carbaldehyde for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.53-8.59 (m, 2H) 8.07 (s, 1H) 7.73 (d, J=9.16 Hz, 2H) 7.10 (d, J=5.49 Hz, 1H) 6.97-7.02 (m, 2H) 4.80-4.87 (m, 4H) 4.03 (d, J=11.60 Hz, 1H) 3.77-3.84 (m, 1H) 3.61-3.69 (m, 1H) 2.88 (d, J=41.81 Hz, 2H) 2.25-2.63 (m, 4H) 1.97 (s, 2H) 1.77-1.91 (m, 4H) 1.64-1.76 (m, 2H) 1.44-1.58 (m, 1H); MS (APCI(+)) m/e 423 (M+H)⁺.

Example 1413 N-(4-{[1-(2-methylpropyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 429, substituting isobutyraldehyde for isobutyraldehyde and N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-(1,2,3,6-tetrahydropyridin-4-yl)phenyl)isoindoline-2-carboxamide. ¹H NMR (400 MHz, Pyridine-d₅. Temp=90° C.) δ ppm 8.49-8.60 (m, 2H) 8.09 (s, 1H) 7.68-7.80 (m, 2H) 7.10 (d, J=5.19 Hz, 1H) 6.96-7.04 (m, 2H) 4.85 (s, 4H) 4.21-4.28 (m, 1H) 2.65-2.79 (m, 2H) 2.13-2.24 (m, 2H) 2.06 (m, 2H) 1.98 (s, 2H) 1.77-1.88 (m, 2H) 1.67-1.77 (m, 1H) 0.89 (d, J=6.71 Hz, 6H); MS (APCI(+)) m/e 395 (M+H)⁺.

Example 1414 N-(4-{[1-(butylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and 1-butylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.59 (s, 1H) 8.49 (d, J=4.88 Hz, 1H) 7.36-7.48 (m, 3H) 6.90 (d, J=8.85 Hz, 2H) 4.80 (d, J=6.10 Hz, 4H) 4.39-4.50 (m, 1H) 3.41-3.49 (m, 2H) 3.13-3.20 (m, 2H) 2.99-3.06 (m, 2H) 1.94-2.01 (m, 2H) 1.63-1.76 (m, 4H) 1.37-1.49 (m, 2H) 0.91 (t, J=7.48 Hz, 3H); MS (APCI(+)) m/e 459 (M+H)⁺.

Example 1415 N-(4-{[1-(cyclopropylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and cyclopropylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.57 (s, 1H) 8.48 (d, J=4.88 Hz, 1H) 7.40 (d, J=8.54 Hz, 3H) 6.90 (d, J=8.85 Hz, 2H) 4.79 (d, J=8.24 Hz, 4H) 4.39-4.49 (m, 1H) 3.44-3.51 (m, 2H) 3.17-3.23 (m, 2H) 2.54-2.58 (m, 1H) 1.95-2.03 (m, 2H) 1.68-1.78 (m, 2H) 0.91-1.07 (m, 4H); MS (APCI(+)) m/e 442 (M+H)⁺.

Example 1416 N-(4-{[1-(phenylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and phenylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.59 (s, 1H) 8.49 (d, J=4.88 Hz, 1H) 7.77 (d, J=7.32 Hz, 2H) 7.71 (t, J=7.32 Hz, 1H) 7.65 (t, J=7.32 Hz, 2H) 7.44 (d, J=4.88 Hz, 1H) 7.35 (d, J=8.85 Hz, 2H) 6.79 (d, J=9.16 Hz, 2H) 4.79 (d, J=4.27 Hz, 4H) 4.29-4.37 (m, 1H) 3.22-3.25 (m, 2H) 2.92-3.06 (m, 2H) 1.87-2.04 (m, 2H) 1.61-1.79 (m, 2H); MS (APCI(+)) m/e 479 (M+H)⁺.

Example 1417 N-[4-({1-[(4-fluorophenyl)sulfonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and (4-fluorophenyl)sulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.58 (s, 1H) 8.49 (d, J=4.88 Hz, 1H) 7.84 (dd, J=8.85, 5.19 Hz, 2H) 7.40-7.49 (m, 3H) 7.36 (d, J=8.85 Hz, 2H) 6.80 (d, J=8.85 Hz, 2H) 4.79 (d, J=4.88 Hz, 4H) 4.28-4.41 (m, 1H) 3.21-3.26 (m, 2H) 2.94-3.05 (m, 2H) 1.89-2.02 (m, 2H) 1.62-1.76 (m, 2H); MS (APCI(+)) m/e 497 (M+H)⁺.

Example 1418 N-(4-{[1-(ethylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and ethylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.58 (s, 1H) 8.48 (d, J=5.19 Hz, 1H) 7.40 (d, J=8.85 Hz, 3H) 6.90 (d, J=8.85 Hz, 2H) 4.79 (d, J=7.32 Hz, 4H) 4.39-4.48 (m, 1H) 3.41-3.49 (m, 2H) 3.14-3.22 (m, 2H) 3.05 (q, J=7.43 Hz, 2H) 1.94-2.03 (m, 2H) 1.64-1.78 (m, 2H) 1.24 (t, J=7.32 Hz, 3H); MS (APCI(+)) m/e 431 (M+H)⁺.

Example 1419 N-(4-{[1-(propan-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and isopropylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.59 (s, 1H) 8.49 (d, J=5.19 Hz, 1H) 7.36-7.47 (m, 3H) 6.89 (d, J=8.85 Hz, 2H) 4.80 (d, J=5.49 Hz, 4H) 4.40-4.49 (m, 1H) 3.46-3.55 (m, 2H) 3.33-3.36 (m, 1H) 3.15-3.24 (m, 2H) 1.93-2.01 (m, 2H) 1.62-1.74 (m, 2H) 1.25 (d, J=6.71 Hz, 6H); MS (APCI(+)) m/e 445 (M+H)⁺.

Example 1420 N-(4-{[1-(benzylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and benzylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.58 (s, 1H) 8.48 (d, J=4.88 Hz, 1H) 7.31-7.46 (m, 8H) 6.87 (d, J=9.16 Hz, 2H) 4.79 (d, J=7.02 Hz, 4H) 4.38-4.44 (m, 1H) 4.36 (s, 2H) 3.34-3.38 (m, 2H) 3.07-3.16 (m, 2H) 1.82-1.90 (m, 2H) 1.57-1.71 (m, 2H); MS (APCI(+)) m/e 493 (M+H)⁺.

Example 1421 N-(4-{[1-(propylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and 1-propylsulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 3 ppm 8.59 (s, 1H) 8.49 (d, J=4.88 Hz, 1H) 7.35-7.46 (m, 3H) 6.90 (d, J=8.85 Hz, 2H) 4.80 (d, J=5.80 Hz, 4H) 4.39-4.48 (m, 1H) 3.39-3.49 (m, 2H) 3.12-3.22 (m, 2H) 2.96-3.06 (m, 2H) 1.93-2.03 (m, 2H) 1.62-1.79 (m, 4H) 1.01 (t, J=7.48 Hz, 3H); MS (APCI(+)) m/e 445 (M+H)⁺.

Example 1422 N-(4-{[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 883, substituting N-(4-(piperidin-4-yloxy)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for N-(4-aminophenyl)isoindoline-2-carboxamide and thiophene-2-sulfonyl chloride for (3-methoxyphenyl)methanesulfonyl chloride. ¹H NMR (400 MHz, DMSO-D₂O, Temp=90° C.) 6 ppm 8.58 (s, 1H) 8.49 (d, J=5.19 Hz, 1H) 7.96 (d, J=4.27 Hz, 1H) 7.63 (d, J=3.05 Hz, 1H) 7.44 (d, J=4.88 Hz, 1H) 7.37 (d, J=8.85 Hz, 2H) 7.23-7.30 (m, 1H) 6.81 (d, J=8.85 Hz, 2H) 4.79 (d, J=4.88 Hz, 4H) 4.29-4.43 (m, 1H) 3.31-3.38 (m, 2H) 2.97-3.09 (m, 2H) 1.93-2.06 (m, 2H) 1.65-1.81 (m, 2H); MS (APCI(+)) m/e 485 (M+H)⁺.

Example 1441 benzyl trans-3-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]cyclobutanecarboxylate Example 1441A benzyl trans-3-(tert-butoxycarbonylamino)cyclobutanecarboxylate

A suspension of trans-3-(tert-butoxycarbonylamino)cyclobutanecarboxylic acid (0.5 g, 2.323 mmol) and potassium carbonate (0.321 g, 2.323 mmol) in dimethylformamide (2.323 ml) was treated with (bromomethyl)benzene (0.401 g, 2.346 mmol) added from a syringe over 3 minutes. The reaction mixture was stirred at room temperature for 17 hours and water was added. The suspension was filtered and the solid collected was washed with water and dried under vacuum to give the title compound.

Example 1441B trans-benzyl 3-aminocyclobutanecarboxylate

The title compound was prepared as described in Example 2D, substituting benzyl trans-3-(tert-butoxycarbonylamino)cyclobutanecarboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2 carboxamido)benzamido)methyl)benzylcarbamate.

Example 1441C benzyl trans-3-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]cyclobutanecarboxylate

The title compound was prepared as described in Example 272B, substituting trans-benzyl 3-aminocyclobutanecarboxylate for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.56 (s, 1H), 8.47 (d, J=5.0 Hz, 1H), 7.43-7.31 (m, 6H), 6.68 (d, J=7.6 Hz, 1H), 5.14 (s, 2H), 4.65-4.58 (m, 4H), 4.41-4.29 (m, 1H), 3.11-2.99 (m, 1H), 2.46-2.25 (m, 4H); MS (ESI(+)) m/e 352 (M+H)⁺.

Example 1452 N-(4-{3-[(3-methylbutanoyl)amino]oxetan-3-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1452A 2-methyl-N-(oxetan-3-ylidene)propane-2-sulfinamide

To a 250 mL round-bottomed flask was added 2-methylpropane-2-sulfinamide (3.36 g, 27.8 mmol) followed by tetraethoxytitanium (11.64 ml, 55.5 mmol) to a tetrahydrofuran (69.4 ml) solution of oxetan-3-one (2 g, 27.8 mmol) at room temperature. The mixture was stirred at 50° C. for 5 hours, cooled and poured into brine. The suspension was filtered through a pad of diatomaceous earth eluting with ethyl acetate. The organics were combined, dried with sodium sulfate, filtered and concentrated under vacuum. The residue was purified by regular phase flash column chromatography to give the title compound.

Example 1452B N-(3-(4-bromophenyl)oxetan-3-yl)-2-methylpropane-2-sulfinamide

To a 50 mL round-bottomed flask was added 1,4-dibromobenzene (2.85 g, 12.07 mmol) in tetrahydrofuran (40.2 ml). The solution was cooled to −78° C. and n-butyl lithium (4.51 ml, 11.26 mmol) was added dropwise. The mixture was stirred for 1 hour at −78° C. 2-methyl-N-(oxetan-3-ylidene)propane-2-sulfinamide (1.41 g, 8.05 mmol) was added as a tetrahydrofuran solution (ca 1 ml) and the reaction was stirred for 10 minutes and warmed to room temperature. Saturated ammonium chloride was added followed by water and dichloromethane. The aqueous layer was extracted twice with dichloromethane and the combined organics were dried with magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by regular phase, flash column chromatography to give the title compound.

Example 1452C N-(4-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)phenyl)acetamide

To a 5 mL microwave tube was added N-(3-(4-bromophenyl)oxetan-3-yl)-2-methylpropane-2-sulfinamide (436 mg, 1.312 mmol), cesium carbonate (1283 mg, 3.94 mmol), and acetamide (116 mg, 1.968 mmol) in dioxane (6.5 ml). Xantphos (76 mg, 0.131 mmol) and tris(dibenzylideneacetone)dipalladium(0) (60.1 mg, 0.066 mmol) were added; the tube was flushed with nitrogen and capped. The mixture was heated at 100° C. for 45 minutes. Aqueous work up with dichloromethane extraction gave an organic layer that was dried with sodium sulfate, filtered and concentrated under vacuum. Regular phase chromatography provided the title compound.

Example 1452D N-(3-(4-aminophenyl)oxetan-3-yl)-2-methylpropane-2-sulfinamide

Claisen's alkali (potassium hydroxide, 12.7 g in 9 ml water and 33 ml methanol) was added to N-(4-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)phenyl)acetamide (300 mg, 0.966 mmol) and the reaction was stirred at 90° C. for 2 hours. The mixture was cooled to room temperature when water and ethyl acetate were added. The aqueous layer was extracted twice with ethyl acetate and the combined organics were dried with magnesium sulfate, filtered and concentrated under vacuum. The residue was purified by regular phase flash column chromatography to give the title compound.

Example 1452E N-(4-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 272B, substituting N-(3-(4-aminophenyl)oxetan-3-yl)-2-methylpropane-2-sulfinamide for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate hydrochloride.

Example 1452F N-(4-(3-aminooxetan-3-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

In a 20 mL vial was added N-(4-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide (253 mg, 0.610 mmol) and methanol (6.1 ml). 4N HCl in dioxane (229 μl, 0.916 mmol) was added and the reaction was stirred for 2 hours. The mixture was concentrated under vacuum to give the title compound which was used without further purification.

Example 1452G N-(4-{3-[(3-methylbutanoyl)amino]oxetan-3-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(3-aminooxetan-3-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and 3-methylbutanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.84 (s, 1H), 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.44 (s, 1H), 7.54 (d, J=8.7 Hz, 2H), 7.43 (d, J=4.8 Hz, 1H), 7.36 (d, J=8.8 Hz, 2H), 4.81 (d, J=6.5 Hz, 6H), 4.69 (d, J=6.5 Hz, 2H), 2.10-1.87 (m, 3H), 0.90 (d, J=6.4 Hz, 6H); MS (ESI(+)) m/e 395 (M+H)⁺.

Example 1453 tert-butyl 4-({4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}sulfonyl)piperidine-1-carboxylate Example 1453A tert-butyl 4-(4-aminophenylthio)piperidine-1-carboxylate

To a 100 mL round-bottomed flask was added 4-aminobenzenethiol (4.9 g, 39.1 mmol) and potassium carbonate (9.72 g, 70.3 mmol) in dimethylformamide (20 ml). tert-Butyl 4-(tosyloxy)piperidine-1-carboxylate (5 g, 14.07 mmol) was added and the reaction was stirred in a sealed flask at 70° C. for 20 hours. The mixture was cooled and filtered through a plug of silica gel with dichloromethane. The filtrate was concentrated under vacuum and chromatographed to give the title compound.

Example 1453B tert-butyl 4-(4-acetamidophenylthio)piperidine-1-carboxylate

To a 10 mL round-bottomed flask was added tert-butyl 4-(4-aminophenylthio)piperidine-1-carboxylate (100 mg, 0.324 mmol) and triethylamine (249 μl, 1.783 mmol) in dichloromethane (3242 μl). The mixture was cooled to −78° C. and acetyl chloride (115 μl, 1.621 mmol) was added. The solution was warmed to room temperature, stirred for 1 h and then diluted with water and additional dichloromethane. The aqueous phase was extracted twice with dichloromethane and the combined organics were dried with sodium sulfate, filtered and concentrated to give the title compound.

Example 1453C tert-butyl 4-(4-acetamidophenylsulfonyl)piperidine-1-carboxylate

In a 10 mL round-bottomed flask was added tert-butyl 4-(4-acetamidophenylthio)piperidine-1-carboxylate (100 mg, 0.285 mmol) in dichloromethane (2.9 ml). The solution was cooled to −20° C. and mCPBA (192 mg, 0.856 mmol) was added. The reaction mixture was allowed to warm to room temperature and treated with 1N aqueous NaOH. The aqueous layer was extracted with dichloromethane and the combined organics were dried with sodium sulfate, filtered and concentrated to give the title compound.

Example 1453D tert-butyl 4-(4-aminophenylsulfonyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 1452D, substituting tert-butyl 4-(4-acetamidophenylsulfonyl)piperidine-1-carboxylate for N-(4-(3-(1,1-dimethylethylsulfinamido)oxetan-3-yl)phenyl)acetamide.

Example 1453E tert-butyl 4-({4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}sulfonyl)piperidine-1-carboxylate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(4-aminophenylsulfonyl)piperidine-1-carboxylate for 4-amino-N-propylbenzamide and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for methyl isoindoline-5-carboxylate. ¹H NMR (300 MHz, DMSO-d₆) δ 8.95 (s, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 7.90-7.83 (m, 2H), 7.76-7.69 (m, 2H), 7.44 (d, J=5.1 Hz, 1H), 4.93-4.76 (m, 4H), 4.09-3.93 (m, 2H), 2.84-2.56 (m, 1H), 1.83 (d, J=10.8 Hz, 1H), 1.48-1.16 (m, 6H); MS (ESI(+)) m/e 431 (M+H)⁺.

Example 1454 N-{4-[4-(propylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1454A 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)piperidine-4-carboxylic acid

The title compound was prepared as described in Example 1246, substituting methyl piperidine-4-carboxylate for methyl azetidine-3-carboxylate hydrochloride in Example 1246A.

Example 1454B N-{4-[4-(propylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting propan-1-amine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)piperidine-4-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.19 (s, 1H), 7.77 (t, J=5.6 Hz, 1H), 7.42 (d, J=5.1 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), 4.77 (d, J=6.2 Hz, 4H), 3.64-3.56 (m, 2H), 3.05-2.94 (m, 2H), 2.63-2.52 (m, 2H), 2.28-2.14 (m, 1H), 1.79-1.59 (m, 4H), 1.47-1.33 (m, 2H), 0.84 (t, J=7.4 Hz, 3H); MS (ESI(+)) m/e 408 (M+H)⁺.

TABLE 23 The following examples were essentially prepared as described in Example 1C, substituting the appropriate amine for 3-phenylpropan-1-amine and 1-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine- 2-carboxamido)phenyl)piperidine-4-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. Ex Name ¹H NMR MS 1455 N-(4-{4-[(2- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm 8.57 (s, (ESI(+)) methoxyethyl)carbamoyl]pi- 1H), 8.47 (d, J = 5.0 Hz, 1H), 7.91 (s, 1H), 7.47-7.41 (m, m/e 424 peridin-1-yl}phenyl)- 1H), 7.40-7.30 (m, 3H), 6.86-6.80 (m, 2H), 4.80-4.74 (M + H)⁺ 1,3-dihydro-2H- (m, 4H), 3.61-3.52 (m, 2H), 3.36 (t, J = 5.9 Hz, 2H), 3.28- pyrrolo[3,4-c]pyridine-2- 3.17 (m, 5H), 2.64 (td, J = 11.7, 3.2 Hz, 2H), 2.32-2.20 (m, carboxamide 1H), 1.82-1.63 (m, 4H) 1456 N-(4-{4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) [(cyclopentylmethyl)carbamoyl]pi- 5.0 Hz, 1H), 8.19 (s, 1H), 7.79 (t, J = 5.7 Hz, 1H), 7.42 (d, J = m/e 448 peridin-1- 5.0 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), 4.80- (M + H)⁺ yl}phenyl)-1,3-dihydro- 4.74 (m, 4H), 3.64-3.56 (m, 2H), 3.01-2.94 (m, 2H), 2H-pyrrolo[3,4- 2.64-2.53 (m, 2H), 2.30-2.16 (m, 1H), 2.04-1.91 (m, c]pyridine-2- 1H), 1.74-1.43 (m, 10H), 1.29-1.06 (m, 2H) carboxamide 1457 N-(4-{4-[(1,4-dioxan-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) ylmethyl)carbamoyl]piperidin- 5.0 Hz, 1H), 8.19 (s, 1H), 7.90 (t, J = 5.8 Hz, 1H), 7.42 (d, J = m/e 466 1-yl}pheny1)-1,3- 5.1 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), 4.78- (M + H)⁺ dihydro-2H-pyrrolo[3,4- 4.74 (m, 4H), 3.75-3.41 (m, 8H), 3.21-3.13 (m, 1H), c]pyridine-2- 3.13-3.02 (m, 2H), 2.63-2.53 (m, 2H), 2.30-2.20 (m, carboxamide 1H), 1.77-1.59 (m, 4H) 1458 N-{4-[4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) (cyclopentylcarbamoyl)piperidin- 5.0 Hz, 1H), 8.19 (s, 1H), 7.73 (d, J = 7.2 Hz, 1H), 7.42 (d, m/e 434 1-yl]phenyl}- J = 5.1 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 4.82-4.71 (m, 4H), 4.04-3.92 (m, 1H), 3.64-3.56 (m, pyrrolo[3,4-c]pyridine-2- 2H), 2.61-2.51 (m, 2H), 2.24-2.13 (m, 1H), 1.84-1.56 carboxamide (m, 8H), 1.55-1.42 (m, 2H), 1.40-1.29 (m, 2H) 1459 N-{4-[4-(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-d₆, Temp = 90° C.) δ ppm 8.57 (s, (ESI(+)) pyran-4- 1H), 8.47 (d, J = 5.0 Hz, 1H), 7.91 (s, 1H), 7.41-7.31 (m, m/e 450 ylcarbamoyl)piperidin-1- 4H), 6.86-6.80 (m, 2H), 4.80-4.74 (m, 4H), 3.85-3.71 (M + H)⁺ yl]phenyl}-1,3-dihydro- (m, 3H), 3.62-3.53 (m, 2H), 3.41-3.29 (m, 2H), 2.70- 2H-pyrrolo[3,4- 2.58 (m, 2H), 2.28-2.18 (m, 1H), 1.81-1.64 (m, 6H), 1.49- c]pyridine-2- 1.36 (m, 2H) carboxamide 1460 N-{4-[4-(morpholin-4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) ylcarbonyl)piperidin-1- 5.0 Hz, 1H), 8.19 (s, 1H), 7.42 (d, J = 5.1 Hz, 1H), 7.39- m/e 436 yl]phenyl}-1,3-dihydro- 7.33 (m, 2H), 6.89-6.83 (m, 2H), 4.81-4.72 (m, 4H), 3.65- (M + H)⁺ 2H-pyrrolo[3,4- 3.42 (m, 10H), 2.79-2.59 (m, 3H), 1.73-1.64 (m, 4H) c]pyridine-2- carboxamide 1461 N-(4-{4-[(tetrahydro-2H- ¹H NMR (400 MHz, DMSO-dg) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) pyran-4- 5.0 Hz, 1H), 8.19 (s, 1H), 7.81 (t, J = 5.8 Hz, 1H), 7.42 (d, J = m/e 464 ylmethyl)carbamoyl]piperidin- 5.1 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), 4.80- (M + H)⁺ 1-yl}pheny1)-1,3- 4.74 (m, 4H), 3.87-3.79 (m, 2H), 3.64-3.56 (m, 2H), dihydro-2H-pyrrolo[3,4- 3.28-3.18 (m, 2H), 2.95 (t, J = 6.2 Hz, 2H), 2.64-2.52 (m, c]pyridine-2- 2H), 2.29-2.18 (m, 1H), 1.78-1.56 (m, 5H), 1.57-1.47 carboxamide (m, 2H), 1.20-1.06 (m, 2H) 1462 N-{4-[4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) (cyclopropylcarbamoyl)piperidin- 5.0 Hz, 1H), 8.19 (s, 1H), 7.84 (d, J = 4.3 Hz, 1H), 7.42 (d, m/e 406 1-yl]phenyl}- J = 5.1 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), (M + H)⁺ 1,3-dihydro-2H- 4.80-4.74 (m, 4H), 3.63-3.55 (m, 2H), 2.66-2.48 (m, pyrrolo[3,4-c]pyridine-2- 3H), 2.20-2.08 (m, 1H), 1.76-1.58 (m, 4H), 0.63-0.55 carboxamide (m, 2H), 0.41-0.33 (m, 2H) 1463 N-(4-{4- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.59 (s, 1H), 8.49 (d, J = (ESI(+)) [(tetrahydrofuran-3- 5.0 Hz, 1H), 8.19 (s, 1H), 7.91 (t, J = 5.7 Hz, 1H), 7.42 (d, J = m/e 450 ylmethyl)carbamoyl]piperidin- 4.5 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), 4.80- (M + H)⁺ 1-yl}pheny1)-1,3- 4.74 (m, 4H), 3.73-3.54 (m, 5H), 3.40-3.34 (m, 1H), dihydro-2H-pyrrolo[3,4- 3.09-2.98 (m, 2H), 2.64-2.53 (m, 2H), 2.37-2.27 (m, c]pyridine-2- 1H), 2.27-2.17 (m, 1H), 1.94-1.83 (m, 1H), 1.79-1.61 carboxamide (m, 4H), 1.57-1.46 (m, 1H) 1464 N-(4-{4-[(2-hydroxy-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) methylpropyl)carbamoyl]piperidin- 5.0 Hz, 1H), 8.19 (s, 1H), 7.66 (t, J = 6.0 Hz, 1H), 7.42 (d, J = m/e 438 1-yl}phenyl)- 4.6 Hz, 1H), 7.39-7.33 (m, 2H), 6.90-6.83 (m, 2H), 4.83- (M + H)⁺ 1,3-dihydro-2H- 4.71 (m, 4H), 4.44 (s, 1H), 3.65-3.57 (m, 2H), 3.03 (d, J = pyrrolo[3,4-c]pyridine-2- 6.0 Hz, 2H), 2.64-2.53 (m, 2H), 2.39-2.27 (m, 1H), 1.79- carboxamide 1.61 (m, 4H), 1.04 (s, 6H) 1465 N-{4-[4-(butan-2- ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.60 (s, 1H), 8.49 (d, J = (ESI(+)) ylcarbamoyl)piperidin-1- 5.0 Hz, 1H), 8.19 (s, 1H), 7.56 (d, J = 8.2 Hz, 1H), 7.42 (d, m/e 422 yl]phenyl}-1,3-dihydro- J = 4.5 Hz, 1H), 7.39-7.33 (m, 2H), 6.89-6.83 (m, 2H), (M + H)⁺ 2H-pyrrolo[3,4- 4.81-4.70 (m, 4H), 3.72-3.54 (m, 3H), 2.62-2.50 (m, c]pyridine-2- 2H), 2.27-2.14 (m, 1H), 1.78-1.58 (m, 4H), 1.44-1.28 carboxamide (m, 2H), 1.01 (d, J = 6.6 Hz, 3H), 0.81 (t, J = 7.4 Hz, 3H)

Example 1472 N-(4-{(4R)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

A racemic mixture of N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide (250 mg) was dissolved in methanol and separated using SCF-LC with a ChiralPak AD-H 21×250 mm column to provide N-(4-{(4R)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.41 (s, 1H), 7.66 (d, J=7.6 Hz, 1H), 7.56-7.48 (m, 2H), 7.43 (d, J=5.1 Hz, 1H), 7.37-7.29 (m, 2H), 6.02 (bs, 1H), 4.84-4.77 (m, 4H), 3.89-3.73 (m, 1H), 2.44 (ddd, J=12.7, 8.7, 4.6 Hz, 2H), 2.41-2.26 (m, 2H), 2.14-1.97 (m, 1H), 1.93-1.81 (m, 1H), 1.67-1.49 (m, 1H), 1.00 (dd, J=6.8, 2.4 Hz, 6H); MS (ESI(+)) m/e 405 (M+H)⁺.

Example 1473 N-(4-{(4S)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

A racemic mixture of N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide (250 mg) was dissolved in methanol and separated using SCF-LC with a ChiralPak AD-H 21×250 mm column to provide N-(4-{(4S)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.41 (s, 1H), 7.66 (d, J=7.6 Hz, 1H), 7.56-7.49 (m, 2H), 7.43 (d, J=5.1 Hz, 1H), 7.37-7.29 (m, 2H), 6.05-5.99 (m, 1H), 4.84-4.77 (m, 4H), 3.89-3.73 (m, 1H), 2.47-2.39 (m, 1H), 2.41-2.30 (m, 2H), 2.11-1.97 (m, 1H), 1.93-1.82 (m, 1H), 1.67-1.50 (m, 1H), 1.00 (dd, J=6.8, 2.4 Hz, 6H); MS (ESI(+)) m/e 405 (M+H)⁺.

Example 1474 N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide Example 1474A tert-butyl 3-(2-hydroxyethyl)azetidine-1-carboxylate

A solution of 2-(1-(tert-butoxycarbonyl)azetidin-3-yl)acetic acid (1 g, 4.65 mmol) in tetrahydrofuran (5 ml) was cooled to 0° C. and treated with borane tetrahydrofuran complex (7.00 ml, 7 mmol) dropwise by syringe. After 1 hour at 0° C. the solution was allowed to warm to room temperature and stirred overnight and then it was quenched with 20 ml of 1M aqueous NaOH. The separated aqueous layer was extracted with ether (2×15 ml), dried with magnesium sulfate, filtered and concentrated to give the title compound which was used without purification.

Example 1474B tert-butyl 3-(2-oxoethyl)azetidine-1-carboxylate

To a solution of oxalyl chloride (488 μl, 5.58 mmol) in 40 ml dichloromethane at −78° C. was added dimethyl sulfoxide (792 μl, 11.16 mmol) dropwise by syringe. The mixture was stirred for 15 minutes at −78° C. when a solution of tert-butyl 3-(2-hydroxyethyl)azetidine-1-carboxylate (936 mg, 4.65 mmol) in 10 ml dichloromethane was added dropwise by syringe. After 1 hour at −78° C., triethylamine (3241 μl, 23.25 mmol) was added and the suspension was warmed to room temperature and stirred for an additional hour. The mixture was quenched with water (25 ml) and saturated aqueous potassium carbonate (10 ml), stirred vigorously and separated. The aqueous layer was extracted with dichloromethane (2×20 ml) and the combined organic layers were dried with magnesium sulfate, filtered and concentrated. The crude material was flash chromatographed to give the title compound.

Example 1474C tert-butyl 3-(3-cyanoallyl)azetidine-1-carboxylate

To a solution of potassium tert-butoxide, 1M in tetrahydrofuran (3694 μl, 3.69 mmol) at 0° C. was added dropwise by syringe a solution of diethyl cyanomethylphosphonate (570 μl, 3.52 mmol) in 5 ml tetrahydrofuran. The reaction mixture was warmed to room temperature and then cooled to 0° C. again. This solution was treated with tert-butyl 3-(2-oxoethyl)azetidine-1-carboxylate (701 mg, 3.52 mmol) in 2 ml tetrahydrofuran dropwise by syringe and then allowed to warm to room temperature. After stirring overnight the gelatinous mixture was quenched with water (20 ml) and extracted with ethyl acetate (2×20 ml); the organic layers were washed with brine (20 ml), dried with magnesium sulfate, filtered and concentrated. The liquid residue was flash chromatographed to give the title compound as a 1:1 mixture of E/Z isomers.

Example 1474D tert-butyl 3-(4-aminobutyl)azetidine-1-carboxylate

7M NH₃—CH₃OH (10 mL) was added to tert-butyl 3-(3-cyanoallyl)azetidine-1-carboxylate (640 mg, 2.88 mmol) and Ra—Ni 2800, water slurry (881 mg, 6.75 mmol) in a 20 mL pressure bottle. The mixture was stirred under 30 psi of hydrogen at room temperature for 16 hours. The mixture was filtered through a polypropylene membrane, concentrated by rotovap and dried under vacuum to provide the title compound which was used without purification.

Example 1474E tert-butyl 3-(4-(isoindoline-2-carboxamido)butyl)azetidine-1-carboxylate

The title compound was prepared as described in Example 344A, substituting tert-butyl 3-(4-aminobutyl)azetidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate.

Example 1474F N-(4-(azetidin-3-yl)butyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 3-(4-(isoindoline-2-carboxamido)butyl)azetidine-1-carboxylate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1474G N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(4-(azetidin-3-yl)butyl)isoindoline-2-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 7.67-7.57 (m, 2H), 7.57-7.39 (m, 3H), 7.39-7.23 (m, 4H), 6.28 (s, 1H), 4.56 (s, 4H), 4.34 (t, J=8.3 Hz, 1H), 4.11 (t, J=9.0 Hz, 1H), 4.01-3.82 (m, 1H), 3.65 (dd, J=9.8, 5.8 Hz, 1H), 3.07 (dd, J=12.7, 6.8 Hz, 2H), 2.66-2.53 (m, 1H), 1.59 (dd, J=15.3, 7.7 Hz, 2H), 1.51-1.36 (m, 2H), 1.25 (dd, J=13.5, 6.4 Hz, 2H); MS (ESI(+)) m/e 378 (M+H)⁺.

Example 1475 N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1475A tert-butyl 3-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)butyl)azetidine-1-carboxylate

The title compound was prepared as described in Example 344A, substituting ten-butyl 3-(4-aminobutyl)azetidine-1-carboxylate for tert-butyl 5-aminoisoindoline-2-carboxylate and 1,3-dihydro-2H-pyrrolo[3,4-c]pyridine for isoindoline.

Example 1475B N-(4-(azetidin-3-yl)butyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 3-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)butyl)azetidine-1-carboxylate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1475C N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 278, substituting benzoyl chloride for acetyl chloride and N-(4-(azetidin-3-yl)butyl)-1H-pyrrolo[3,4-c]pyridine-2 (3H)-carboxamide for 5-amino-N-(4-(propylcarbamoyl)phenyl)isoindoline-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.55 (s, 1H), 8.46 (d, J=5.0 Hz, 1H), 7.67-7.55 (m, 2H), 7.55-7.34 (m, 4H), 6.37 (t, J=5.5 Hz, 1H), 4.60 (d, J=2.3 Hz, 4H), 4.35 (t, J=8.3 Hz, 1H), 4.11 (t, J=9.1 Hz, 1H), 3.96-3.83 (m, 1H), 3.65 (dd, J=9.7, 5.7 Hz, 1H), 3.07 (dd, J=12.8, 6.7 Hz, 2H), 2.65-2.53 (m, 1H), 1.59 (dd, J=15.2, 7.6 Hz, 2H), 1.43 (dd, J=14.4, 7.2 Hz, 2H), 1.34-1.09 (m, 2H); MS (ESI(+)) m/e 379 (M+H)⁺.

Example 1476 N-[trans-3-(benzylcarbamoyl)cyclobutyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1476A trans-3-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)cyclobutanecarboxylic acid

The title compound was prepared as described in Example 272A, substituting benzyl trans-3-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]cyclobutanecarboxylate for 4-nitro-N-propylbenzamide.

Example 1476B N-[trans-3-(benzylcarbamoyl)cyclobutyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting benzylamine for 3-phenylpropan-1-amine and trans-3-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)cyclobutanecarboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.56 (s, 1H), 8.47 (d, J=5.0 Hz, 1H), 8.26 (t, J=5.9 Hz, 1H), 7.39 (d, J=5.1 Hz, 1H), 7.36-7.28 (m, 2H), 7.27-7.20 (m, 3H), 6.60 (d, J=7.6 Hz, 1H), 4.65-4.59 (m, 4H), 4.45-4.29 (m, 1H), 4.28 (d, J=5.9 Hz, 2H), 2.96-2.84 (m, 1H), 2.41-2.29 (m, 2H), 2.30-2.15 (m, 2H); MS (ESI(+)) m/e 351 (M+H)⁺.

Example 1477 N-{trans-3-[(2-phenylethyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 2-phenylethylamine for 3-phenylpropan-1-amine and trans-3-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)cyclobutanecarboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.56 (s, 1H), 8.47 (d, J=5.0 Hz, 1H), 7.80 (t, J=5.6 Hz, 1H), 7.39 (d, J=5.1 Hz, 1H), 7.33-7.24 (m, 2H), 7.23-7.16 (m, 3H), 6.57 (d, J=7.6 Hz, 1H), 4.65-4.58 (m, 4H), 4.38-4.24 (m, 1H), 3.33-3.23 (m, 2H), 2.84-2.74 (m, 1H), 2.72 (t, J=7.3 Hz, 2H), 2.32-2.22 (m, 2H), 2.24-2.09 (m, 2H); MS (ESI(+)) m/e 365 (M+H)⁺.

Example 1478 N-{trans-3-[(3-phenylpropyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting 3-phenylpropylamine for 3-phenylpropan-1-amine and trans-3-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)cyclobutanecarboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (400 MHz, DMSO-d₆) δ ppm 8.56 (s, 1H), 8.47 (d, J=5.0 Hz, 1H), 7.75 (t, J=5.5 Hz, 1H), 7.38 (d, J=5.1 Hz, 1H), 7.32-7.24 (m, 2H), 7.24-7.13 (m, 3H), 6.58 (d, J=7.6 Hz, 1H), 4.66-4.55 (m, 4H), 4.41-4.27 (m, 1H), 3.11-3.03 (m, 2H), 2.89-2.75 (m, 1H), 2.62-2.52 (m, 2H), 2.39-2.25 (m, 2H), 2.26-2.11 (m, 2H), 1.76-1.63 (m, 2H); MS (ESI(+)) m/e 379 (M+H)⁺.

Example 1525 N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1525A tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)cyclohexylcarbamate

The title compound was prepared as described in Example 979A, substituting tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)cyclohex-3-enylcarbamate for tert-Butyl 4-(4-(isoindoline-2-carboxamido)phenyl)-5,6-dihydropyridine-1(2H)-carboxylate.

Example 1525B N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)phenyl)cyclohexylcarbamate for tert-butyl 4-((4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1525C N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and 2-(2-methoxyethoxy)acetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (501 MHz, DMSO-d₆) δ 8.59 (bs, 1H), 8.51-8.45 (m, 1H), 8.32 (bs, 1H), 7.44 (dd, J=11.5, 5.2 Hz, 3H), 7.40 (t, J=7.6 Hz, 1H), 7.17-7.11 (m, 2H), 4.81-4.74 (m, 4H), 4.03-3.96 (m, 1H), 3.90 (d, J=2.2 Hz, 2H), 3.63-3.58 (m, 2H), 3.52-3.46 (m, 2H), 3.27-3.23 (m, 3H), 1.80-1.30 (m, 8H); MS (ESI(+)) m/e 453 (M+H)⁺.

Example 1526 N-[4-(trans-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and 2-(2-methoxyethoxy)acetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-[4-(trans-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (501 MHz, DMSO-d₆) δ 8.58 (s, 1H), 8.48 (d, J=5.0 Hz, 1H), 8.31 (s, 1H), 7.50-7.39 (m, 4H), 7.15-7.09 (m, 2H), 4.81-4.74 (m, 4H), 3.85 (s, 2H), 3.74-3.58 (m, 1H), 3.58-3.55 (m, 2H), 3.49-3.46 (m, 2H), 3.28 (s, 3H), 2.45-2.37 (m, 1H), 1.89-1.82 (m, 2H), 1.83-1.75 (m, 2H), 1.58-1.42 (m, 2H), 1.44-1.29 (m, 2H); MS (ESI(+)) m/e 453 (M+H)⁺.

Example 1527 N-[4-(cis-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and (S)-tetrahydrofuran-2-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-[4-(cis-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (501 MHz, DMSO-d₆) δ 8.59 (s, 1H), 8.48 (d, J=5.0 Hz, 1H), 8.32 (s, 1H), 7.47-7.38 (m, 4H), 7.17-7.12 (m, 2H), 4.81-4.75 (m, 4H), 4.29-4.22 (m, 1H), 3.94-3.86 (m, 2H), 3.77 (t, J=7.1 Hz, 1H), 2.14-2.02 (m, 1H), 1.88-1.78 (m, 3H), 1.70 (dd, J=22.1, 8.6 Hz, 3H), 1.63 (t, J=17.3 Hz, 6H); MS (ESI(+)) m/e 435 (M+H)⁺.

Example 1528 N-[4-(trans-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and (S)-tetrahydrofuran-2-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-[4-(trans-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (501 MHz, DMSO-d₆) δ 8.58 (bs, 1H), 8.51-8.45 (m, 1H), 8.30 (bs, 1H), 7.53-7.45 (m, 1H), 7.42 (d, J=8.3 Hz, 2H), 7.14-7.08 (m, 2H), 4.81-4.74 (m, 4H), 4.20-4.13 (m, 1H), 3.92-3.85 (m, 1H), 3.78-3.71 (m, 1H), 3.66-3.58 (m, 1H), 2.39 (s, 1H), 2.09 (dd, J=10.8, 6.4 Hz, 1H), 1.79 (s, 7H), 1.62 (s, 1H), 1.45 (dd, J=26.5, 15.7 Hz, 4H); MS (ESI(+)) m/e 435 (M+H)⁺.

Example 1529 N-[4-(cis-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and (R)-tetrahydrofuran-2-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-[4-(cis-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (501 MHz, DMSO-d₆) δ 8.55 (t, J=21.5 Hz, 1H), 8.46 (s, 1H), 8.32 (d, J=9.4 Hz, 1H), 7.47-7.37 (m, 4H), 7.14 (bs, 2H), 4.77 (bs, 4H), 4.29-4.20 (m, 1H), 3.96-3.84 (m, 2H), 3.80-3.71 (m, 1H), 2.12-2.01 (m, 1H), 1.76 (d, J=48.5 Hz, 4H), 1.60 (s, 7H); MS (ESI(+)) m/e 435 (M+H)⁺.

Example 1530 N-[4-(trans-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and (R)-tetrahydrofuran-2-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-[4-(trans-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (501 MHz, DMSO-d₆) δ 8.58 (bs, 1H), 8.50-8.45 (m, 1H), 8.31 (bs, 1H), 7.52-7.46 (m, 1H), 7.45-7.39 (m, 3H), 7.14-7.08 (m, 2H), 4.81-4.74 (m, 4H), 4.20-4.13 (m, 1H), 3.92-3.84 (m, 1H), 3.78-3.70 (m, 1H), 3.66-3.57 (m, 1H), 2.43-2.34 (m, 1H), 2.14-2.02 (m, 1H), 2.04-1.52 (m, 7H), 1.54-1.24 (m, 4H); MS (ESI(+)) m/e 435 (M+H)⁺.

Example 1531 N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide Example 1531A methyl 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylate

Methyl 6-aminopyridazine-3-carboxylate (2 g, 13.06 mmol) was suspended in dichloromethane (50 ml) followed by addition of dry pyridine (1.265 ml, 15.67 mmol) under nitrogen. To this suspension was added a dichloromethane solution of 4-nitrophenyl carbonochloridate (2.99 g, 14.37 mmol) via syringe at ambient temperature. The mixture was stirred overnight to give a suspension that was concentrated to half volume under a stream of nitrogen. 2,3-Dihydro-1H-pyrrolo[3,4-c]pyridine, dihydrochloride (2.52 g, 13.06 mmol) was dissolved in 30 ml dimethylformamide with triisopropylethylamine (6.84 ml, 39.2 mmol) and added to the carbamate mixture via syringe. After stirring the mixture overnight and removing most of the solvent under vacuum, water was added; and the resulting suspension was stirred for 30 minutes and filtered to give a solid which was washed with water. Flash chromatography of the dried solid gave the title compound.

Example 1531B 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylic acid

The title compound was prepared as described in Example 1B, substituting methyl 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylate for methyl 4-(isoindoline-2-carboxamido)benzoate.

Example 1531C N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (25)-tetrahydrofuran-2-ylmethamine for 3-phenylpropan-1-amine and 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.09 (s, 1H), 8.81 (t, J=6.1 Hz, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 8.31 (d, J=9.3 Hz, 1H), 8.12 (d, J=9.3 Hz, 1H), 7.44 (d, J=5.1 Hz, 1H), 5.05-4.76 (m, 4H), 4.04 (p, J=6.2 Hz, 1H), 3.85-3.74 (m, 1H), 3.70-3.59 (m, 1H), 3.45-3.31 (m, 2H), 1.99-1.72 (m, 3H), 1.69-1.54 (m, 1H); MS (ESI(+)) m/e 369 (M+H)⁺.

Example 1542 N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting (2R)-tetrahydrofuran-2-ylmethamine for 3-phenylpropan-1-amine and 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.09 (bs, 1H), 8.81 (t, J=6.1 Hz, 1H), 8.61 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 8.31 (d, J=9.3 Hz, 1H), 8.12 (d, J=9.3 Hz, 1H), 7.44 (d, J=5.1 Hz, 1H), 5.05-4.76 (m, 4H), 4.04 (p, J=6.2 Hz, 1H), 3.85-3.74 (m, 1H), 3.70-3.59 (m, 1H), 3.35 (d, J=25.7 Hz, 2H), 1.99-1.72 (m, 3H), 1.69-1.54 (m, 1H); MS (ESI(+)) m/e 369 (M+H)⁺.

Example 1543 N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting tetrahydro-2H-pyran-4-ylmethamine for 3-phenylpropan-1-amine and 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.06 (s, 1H), 9.00 (t, J=6.2 Hz, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 8.29 (d, J=9.3 Hz, 1H), 8.11 (d, J=9.3 Hz, 1H), 7.44 (d, J=5.1 Hz, 1H), 4.96-4.89 (m, 4H), 3.89-3.79 (m, 2H), 3.22 (d, J=2.6 Hz, 3H), 1.96-1.75 (m, 1H), 1.64-1.53 (m, 2H), 1.31-1.10 (m, 2H); MS (ESI(+)) m/e 383 (M+H)⁺.

Example 1544 N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting cyclopentylmethamine for 3-phenylpropan-1-amine and 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.03 (bs, 1H), 8.95 (t, J=6.1 Hz, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 8.29 (d, J=9.3 Hz, 1H), 8.11 (d, J=9.3 Hz, 1H), 7.44 (d, J=5.1 Hz, 1H), 4.99-4.75 (m, 4H), 3.28-3.20 (m, 2H), 2.31-2.13 (m, 1H), 1.75-1.38 (m, 6H), 1.39-1.18 (m, 2H); MS (ESI(+)) m/e 367 (M+H)⁺.

Example 1545 N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting tetrahydrofuran-3-ylmethamine for 3-phenylpropan-1-amine and 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.05 (s, 1H), 9.13 (t, J=6.1 Hz, 1H), 8.62 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 8.30 (d, J=9.3 Hz, 1H), 8.12 (d, J=9.3 Hz, 1H), 7.44 (d, J=5.1 Hz, 1H), 5.05-4.76 (m, 4H), 3.80-3.57 (m, 4H), 3.48 (dd, J=12.1, 6.8 Hz, 1H), 3.37-3.31 (m, 1H), 2.62-2.52 (m, 1H), 2.01-1.80 (m, 1H), 1.71-1.56 (m, 1H); MS (ESI(+)) m/e 369 (M+H)⁺.

Example 1546 N-{6-[(bicyclo[2.2.1]hept-2-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C, substituting bicyclo[2.2.1]hept-2-ylmethamine for 3-phenylpropan-1-amine and 6-(2,3-dihydro-1H-pyrrolo[3,4-c]pyridine-2-carboxamido)pyridazine-3-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 10.05 (bs, 1H), 8.92 (d, J=42.7 Hz, 1H), 8.61 (s, 1H), 8.51 (d, J=5.0 Hz, 1H), 8.29 (d, J=9.3 Hz, 1H), 8.10 (d, J=9.3 Hz, 1H), 7.47-7.41 (m, 1H), 5.07-4.74 (m, 4H), 3.23-2.84 (m, 2H), 2.30-2.02 (m, 3H), 1.86-1.57 (m, 2H), 1.58-0.99 (m, 6H); MS (ESI(+)) m/e 393 (M+H)⁺.

Example 1547 N-(4-{trans-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and isobutyric acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-(4-{trans-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.32 (s, 1H), 7.58 (d, J=7.8 Hz, 1H), 7.48-7.40 (m, 3H), 7.17-7.09 (m, 2H), 4.82-4.76 (m, 4H), 3.65-3.47 (m, 1H), 2.41-2.23 (m, 2H), 1.93-1.69 (m, 4H), 1.62-1.38 (m, 2H), 1.39-1.12 (m, 2H), 0.99 (d, J=6.8 Hz, 6H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 1548 N-(4-{cis-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and isobutyric acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-(4-{cis-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.33 (s, 1H), 7.68-7.61 (m, 1H), 7.49-7.40 (m, 3H), 7.21-7.14 (m, 2H), 4.83-4.76 (m, 4H), 3.98-3.90 (m, 1H), 1.97-1.49 (m, 9H), 1.04-0.97 (m, 6H); MS (ESI(+)) m/e 407 (M+H)⁺.

Example 1549 N-(4-{cis-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and cyclohexanecarboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-(4-{cis-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.33 (s, 1H), 7.66-7.59 (m, 1H), 7.47 (s, 1H), 7.47-7.40 (m, 2H), 7.21-7.14 (m, 2H), 4.83-4.76 (m, 4H), 3.98-3.90 (m, 1H), 2.45 (s, 1H), 2.31-2.19 (m, 1H), 1.89-1.46 (m, 12H), 1.46-1.05 (m, 6H); MS (ESI(+)) m/e 447 (M+H)⁺.

Example 1550 N-(4-{trans-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and cyclohexanecarboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-(4-{trans-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.49 (d, J=5.0 Hz, 1H), 8.32 (s, 1H), 7.54 (d, J=7.9 Hz, 1H), 7.47-7.40 (m, 3H), 7.16-7.09 (m, 2H), 4.82-4.75 (m, 4H), 3.62-3.42 (m, 1H), 2.42-2.33 (m, 1H), 2.12-1.99 (m, 1H), 1.87-1.61 (m, 8H), 1.55-1.37 (m, 3H), 1.38-1.08 (m, 7H); MS (ESI(+)) m/e 447 (M+H)⁺.

Example 1551 N-(4-{trans-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and 2-cyclopropylacetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-(4-{trans-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.60 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.32 (s, 1H), 7.59 (d, J=7.8 Hz, 1H), 7.48-7.40 (m, 3H), 7.11 (s, 2H), 4.82-4.76 (m, 4H), 3.66-3.50 (m, 1H), 2.40 (t, J=10.1 Hz, 1H), 1.94 (t, J=11.8 Hz, 1H), 1.83 (dd, J=23.4, 12.2 Hz, 4H), 1.61-1.39 (m, 2H), 1.40-1.18 (m, 3H), 1.04-0.83 (m, 1H), 0.46-0.33 (m, 2H), 0.18-0.07 (m, 2H); MS (ESI(+)) m/e 419 (M+H)⁺.

Example 1552 N-(4-{cis-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide

The title compound was prepared as described in Example 1C as a 1:1 cis/trans mixture, substituting N-(4-(4-aminocyclohexyl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide for 3-phenylpropan-1-amine and 2-cyclopropylacetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. HPLC separation of the cis/trans isomers provided N-(4-{cis-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide. ¹H NMR (300 MHz, DMSO-d₆) δ 8.61 (s, 1H), 8.50 (d, J=5.0 Hz, 1H), 8.33 (s, 1H), 7.67-7.60 (m, 1H), 7.49-7.40 (m, 3H), 7.21-7.13 (m, 2H), 4.83-4.76 (m, 4H), 4.02-3.92 (m, 1H), 2.06 (d, J=7.0 Hz, 2H), 1.84-1.65 (m, 4H), 1.65-1.47 (m, 4H), 1.25-0.90 (m, 1H), 0.47-0.34 (m, 2H), 0.23-0.11 (m, 2H); MS (ESI(+)) m/e 419 (M+H)⁺.

Example 1553 N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide Example 1553A tert-butyl 4-(4-nitrophenyl)cyclohex-3-enylcarbamate

The title was prepared as in Example 1018B, substituting 4,4,5,5-tetramethyl-2-(4-nitrophenyl)-1,3,2-dioxaborolane for N-(4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1H-pyrrolo[3,4-c]pyridine-2(3H)-carboxamide.

Example 1553B tert-butyl 4-(4-aminophenyl)cyclohex-3-enylcarbamate

tert-Butyl 4-(4-nitrophenyl)cyclohex-3-enylcarbamate (2.55 g, 8.01 mmol) was suspended in ethanol (30 ml) followed by addition of sodium sulfide, nonahydrate (10.37 ml, 80 mmol) dissolved in water (30 ml). The mixture was heated to 80° C. for 1.5 h and extracted with dichloromethane; the organic layers were combined, dried over magnesium sulfate, filtered and concentrated to give the title compound.

Example 1553C tert-butyl 4-(4-(isoindoline-2-carboxamido)phenyl)cyclohex-3-enylcarbamate

The title compound was prepared as described in Example 272B, substituting tert-butyl 4-(4-aminophenyl)cyclohex-3-enylcarbamate for 4-amino-N-propylbenzamide and isoindoline for methyl isoindoline-5-carboxylate hydrochloride.

Example 1553D N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide

The title compound was prepared as described in Example 2D, substituting tert-butyl 4-(4-(isoindoline-2-carboxamido)phenyl)cyclohex-3-enylcarbamate for tert-butyl 44(4-(5-fluoroisoindoline-2-carboxamido)benzamido)methyl)benzylcarbamate.

Example 1553E N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and isobutyric acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.36 (s, 1H), 7.70 (d, J=7.6 Hz, 1H), 7.54 (d, J=2.1 Hz, 2H), 7.46-7.23 (m, 6H), 6.06-5.96 (m, 1H), 4.76 (s, 4H), 3.85-3.75 (m, 1H), 2.43-2.26 (m, 3H), 2.11-1.96 (m, 1H), 1.95-1.75 (m, 1H), 1.69-1.48 (m, 1H), 1.10-0.82 (m, 6H); MS (ESI(+)) m/e 404 (M+H)⁺.

Example 1554 N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and -(2R)-tetrahydrofuran-2-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.36 (s, 1H), 7.61 (dt, J=9.2, 4.6 Hz, 1H), 7.58-7.45 (m, 2H), 7.49-7.23 (m, 6H), 6.02 (bs, 1H), 4.77 (s, 4H), 4.25-4.16 (m, 1H), 3.97-3.66 (m, 3H), 2.42-2.24 (m, 1H), 2.26-1.98 (m, 3H), 1.98-1.53 (m, 6H); MS (ESI(+)) m/e 432 (M+H)⁺.

Example 1555 N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and -(25)-tetrahydrofuran-2-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.37 (s, 1H), 7.63 (dd, J=8.2, 3.5 Hz, 1H), 7.57-7.50 (m, 2H), 7.49-7.23 (m, 6H), 6.04-5.96 (m, 1H), 4.76 (s, 4H), 4.25-4.16 (m, 1H), 3.96-3.67 (m, 4H), 2.38-2.29 (m, 1H), 2.27-1.99 (m, 3H), 1.97-1.56 (m, 5H); MS (ESI(+)) m/e 432 (M+H)⁺.

Example 1556 N-(4-{4-[(cyclopentylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and cyclopentylacetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.34 (s, 1H), 7.72 (d, J=7.6 Hz, 1H), 7.57-7.49 (m, 2H), 7.49-7.23 (m, 6H), 6.01 (bs, 1H), 4.76 (s, 4H), 3.90-3.74 (m, 1H), 2.49-2.25 (m, 2H), 2.20-1.99 (m, 3H), 1.94-1.82 (m, 1H), 1.68 (tdd, J=9.4, 8.9, 4.4 Hz, 2H), 1.64-1.42 (m, 7H), 1.31-1.01 (m, 2H); MS (ESI(+)) m/e 444 (M+H)⁺.

Example 1557 N-(4-{4-[(cyclopropylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and cyclopropylacetic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.36 (s, 1H), 7.70 (d, J=7.6 Hz, 1H), 7.66-7.47 (m, 2H), 7.47-7.24 (m, 6H), 6.02 (bs, 1H), 4.76 (s, 4H), 3.88-3.78 (m, 1H), 2.49-2.26 (m, 3H), 2.12-1.82 (m, 4H), 1.72-1.50 (m, 1H), 1.13-0.88 (m, 1H), 0.52-0.33 (m, 2H), 0.18-0.01 (m, 2H); MS (ESI(+)) m/e 416 (M+H)⁺.

Example 1558 N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and 2-hydroxy-2-methylpropanoic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.36 (s, 1H), 7.52 (t, J=8.6 Hz, 2H), 7.46-7.39 (m, 1H), 7.35 (tdd, J=8.8, 7.1, 3.7 Hz, 6H), 6.07-5.96 (m, 1H), 5.40 (s, 1H), 4.77 (s, 4H), 3.92-3.76 (m, 1H), 2.46 (s, 1H), 2.39-2.25 (m, 1H), 2.24-2.09 (m, 2H), 1.93-1.78 (m, 1H), 1.70 (dt, J=12.4, 7.7 Hz, 1H), 1.25 (s, 6H); MS (ESI(+)) m/e 420 (M+H)⁺.

Example 1559 N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-isoindole-2-carboxamide

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and tetrahydro-2H-pyran-4-carboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.36 (s, 1H), 7.76 (d, J=7.6 Hz, 1H), 7.57-7.49 (m, 2H), 7.46-7.23 (m, 6H), 6.02 (bs, 1H), 4.76 (s, 4H), 3.91-3.75 (m, 4H), 3.31-3.17 (m, 2H), 2.43-2.26 (m, 2H), 2.12-1.97 (m, 1H), 1.93-1.81 (m, 1H), 1.71-1.48 (m, 6H); MS (ESI(+)) m/e 446 (M+H)⁺.

The title compound was prepared as described in Example 1C, substituting N-(4-(4-aminocyclohex-1-enyl)phenyl)isoindoline-2-carboxamide for 3-phenylpropan-1-amine and cyclohexanecarboxylic acid for 4-(isoindoline-2-carboxamido)benzoic acid. ¹H NMR (300 MHz, DMSO-d₆) δ 8.35 (s, 1H), 7.64 (d, J=7.6 Hz, 1H), 7.57-7.49 (m, 2H), 7.47-7.23 (m, 6H), 6.01 (bs, 1H), 4.76 (s, 4H), 3.84-3.54 (m, 1H), 2.49-2.24 (m, 2H), 2.20-1.93 (m, 2H), 1.91-1.77 (m, 1H), 1.78-1.48 (m, 6H), 1.47-1.06 (m, 6H); MS (ESI(+)) m/e 444 (M+H)⁺. 

What is claimed is:
 1. A compound of Formula (Ic), or a pharmaceutically acceptable salt thereof

wherein X¹ and X³ are CH; and X² is N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂; R² is alkyl, alkenyl, alkynyl, phenyl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R² alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁴, OR⁴, SR⁴, S(O)R⁴, SO₂R⁴, C(O)R⁴, CO(O)R⁴, OC(O)R⁴, OC(O)OR⁴, NHC(O)R⁴, NR⁴C(O)R⁴, NHS(O)₂R⁴, NR⁴S(O)₂R⁴, NHC(O)OR⁴, NR⁴C(O)OR⁴, NHC(O)NH₂, NHC(O)NHR⁴, NHC(O)N(R⁴)₂, NR⁴C(O)NHR⁴, NR⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R⁴, C(O)NR⁴SO₂R⁴, SO₂NH₂, SO₂NHR⁴, SO₂N(R⁴)₂, C(O)H, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R² phenyl is optionally substituted at the para position with one independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or heterocyclyl; wherein each R⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, NHC(O)R⁷, NR^(T)C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R)₂, NR^(T)C(O)NHR⁷, NR^(T)C(O)N(R)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NRSO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R^(T))₂, C(O)H, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R⁴ aryl and heterocycyl is optionally substituted with one, two, three or four independently selected R⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰OC(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁷, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁷ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, NHR¹¹, N(R¹¹)₂, C(O)R¹¹, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, NHSO₂R¹¹, NHC(O)OR¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, NHC(O)NH₂, NHC(O)NHR¹¹, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁸, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁸ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl; R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; R¹¹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; R¹², at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹² alkyl, alkenyl, and alkynyl is optionally substituted with one or more alkoxy; wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I; R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR⁵, NR¹⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I; wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; with the proviso that when R² is unsubstituted alkyl or optionally substituted alkyl; R² is C₄-C₆-alkyl; and with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.
 2. A compound having Formula (Vc), or a pharmaceutically acceptable salt thereof

wherein X¹ and X³ are CH; and X² is N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂; R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl; R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R³, SO₂R³, C(O)R³, CO(O)R³, OC(O)R³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I; R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I; R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.
 3. A compound having Formula (VIIc), or a pharmaceutically acceptable salt thereof

wherein X¹ and X³ are CH; and X² is N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH;

indicates a single or double bond; R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂; R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the cyclic moieties represented by R³, R⁶, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I; R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I; R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.
 4. A compound having Formula (VIIIc), or a pharmaceutically acceptable salt thereof

wherein X¹ and X³ are CH; and X² is N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂; R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁸, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁸ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹², OR¹², SR¹², S(O)R¹², SO₂R¹², NHR¹², N(R²)₂, C(O)R¹², C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHSO₂R¹², NHC(O)OR¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, NHC(O)NH₂, NHC(O)NHR¹², OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; R¹², at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹² alkyl, alkenyl, and alkynyl is optionally substituted with one or more alkoxy; wherein the cyclic moieties represented by R³, R⁶, R⁸, R¹⁰, and R¹² are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I; R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR¹⁶, OH, F, Cl, Br, or I; wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.
 5. The compound of claim 1, claim 2, claim 3, or claim 4, or a pharmaceutically acceptable salt thereof; wherein X¹ and X³ are CH; and X² is N.
 6. The compound of claim 1, or a pharmaceutically acceptable salt thereof; wherein R² is phenyl which is substituted at the para position with R⁵; and R⁵ is phthalazin-1(2H)-onyl, isoquinolinyl, isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl, 5-fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl, 5-(trifluoromethyl)phthalazin-1(2H)-onyl, pyrrolo[1,2-d][1,2,4]triazin-1(2H)-one, or isoindolin-1-onyl.
 7. The compound of claim 1, selected from the group consisting of: N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(pyridin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(1S)-2-hydroxy-1-phenylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(1 S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(tetrahydrofuran-3-ylmethyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-oxo-3,4-dihydrophthalazin-1-yl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1 S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1 S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-hydroxypiperidin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2 S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(5,6-dihydroimidazo[1,5-a]pyrazin-7(8H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(1′-isobutyryl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(1′-benzoyl-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[1′-(tetrahydrofuran-3-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{1′-[(2-methoxyethoxy)acetyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(morpholin-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[6-(benzoylamino)hexyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[1′-(tetrahydrofuran-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[1′-(tetrahydro-2H-pyran-4-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[1′-(1,4-dioxan-2-ylcarbonyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{1′-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[1′-(2-hydroxy-2-methylpropanoyl)-1′,2′,3′,6′-tetrahydro-2,4′-bipyridin-5-yl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(azetidin-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(2,6-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,7-diazaspiro[4.4]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[methyl(propyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[benzyl(methyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(trifluoromethyl)piperidin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-chlorobenzoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(2-aminoethyl)-1H-imidazol-1-yl]carbonyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazol-5-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-phenylbutyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-methylbutyl)sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylmethyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(cyclopentylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-pentanoylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-acetylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-butyrylpiperidin-4-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-methylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(methoxyacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopropylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopropylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclobutylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclohexylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1 S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydrofuran-3-ylmethyl) sulfamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3,3,3-trifluoropropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(4,4,4-trifluorobutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-3-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclobutylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3-phenylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-hydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(phenylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(4-methoxyphenyl)acetyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(methoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopropylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclohexylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-benzoylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3-ethoxypropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(2-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(1-methylcyclopropyl)carbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-methylpropanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-acetylpyrrolidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(4,4,4-trifluorobutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(ethoxyacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydro-2H-pyran-4-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(morpholin-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(2-methoxyethoxy)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclohexylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-2-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(morpholin-4-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclohexylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-methylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2,2-dimethylpropanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3,3-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tricyclo[3.3.1.1˜3,7˜]dec-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(4-methoxycyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[4-(acetylamino)phenyl]sulfonyl}amino)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(propylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(4-propylphenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(butylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[({[(1 S,4R)-7,7-dimethyl-2-oxobicyclo[2.2.1]hept-1-yl]methyl}sulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(ethylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(benzylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(4-fluorophenyl)sulfonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(thiophen-2-ylsulfonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,7-diazaspiro[4.4]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(2,7-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(2,6-diazaspiro[4.5]dec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(2,7-diazaspiro[4.5]dec-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(2,9-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(2,8-diazaspiro[5.5]undec-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,8-diazaspiro[5.5]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,8-diazaspiro[4.6]undec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-oxa-4,8-diazaspiro[5.5]undec-4-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,8-diazaspiro[4.5]dec-1-ylcarbonyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,8-diazaspiro[4.5]dec-8-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,7-diazaspiro[3.5]non-7-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1,6-diazaspiro[3.5]non-1-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(2,5-diazaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(5-oxa-2-azaspiro[3.4]oct-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(6-oxa-2-azaspiro[3.5]non-2-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(hexahydro-5H-furo[2,3-c]pyrrol-5-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(tetrahydro-1H-furo[3,4-c]pyrrol-5 (3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(hexahydrofuro[3,4-c]pyridin-5(3H)-ylcarbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(N,N-dimethylglycyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydrofuran-2-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydrofuran-3-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(cyclohexylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(4,4-difluorocyclohexyl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(2-hydroxy-2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(piperidin-1-ylsulfonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(5-methyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-({4-[2-(2-hydroxyethoxy)ethyl]piperazin-1-yl}carbonyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-carbamoylbenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[bis(2-methoxyethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[4-(pyrazin-2-yl)piperazin-1-yl]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; Nalpha-{4-[(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-cyclohexylpiperazin-1-yl)carbonyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-(4,5,6,7-tetrahydro-1H-indazol-5-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[methyl(3-methylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-cyanocyclopropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-(butylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[methyl(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-methoxyethyl)(methyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[methyl(propyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; methyl 1-{4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}azetidine-3-carboxylate; N-(4-{3-[(3-methylbutyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{3-[(tetrahydrofuran-2-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{3-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[3-(benzylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[3-(cyclopentylcarbamoyl)azetidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{3-[(cyclopentylmethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{3-[(2-methoxyethyl)carbamoyl]azetidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(pyrrolidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(9-chloro-5-oxo-2,3,3a,4,4a,5-hexahydro-6H-furo[2′,3′:2,3]cyclobuta[1,2-c]quinolin-6-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[7-chloro-1-(2-hydroxyethyl)-3-oxo-1,3-dihydrocyclobuta[c]quinolin-4(2H)-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(cyclopropylacetyl)amino]cyclohexx-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-acetylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-butanoylpiperidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(methoxyacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-methylbutanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3,3,3-trifluoropropanoyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopropylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclobutylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclobutylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydro-2H-pyran-2-ylcarbonyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydro-2H-pyran-4-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-2-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-3-ylacetyl)piperidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(5-oxo-L-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclohexylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopropylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-ethoxypropanoyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1-acetylpiperidin-4-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(ethoxyacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydrofuran-2-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydrofuran-3-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(cyclopentylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(bicyclo[2.2.1]hept-2-ylacetyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1,3-thiazol-5-ylcarbonyl)amino]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(4-oxo-4,5,6,7-tetrahydro-1-benzofuran-3-yl)carbonyl]amino}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(5-oxo-L-prolyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-propanoylazetidin-3-yl)oxy]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2,2-dimethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-ethylbutanoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(pent-4-ynoyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(furan-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(furan-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(thiophen-3-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(pyrimidin-4-ylcarbonyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(N,N-dimethylglycyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(N,N-dimethyl-beta-alanyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(pyrrolidin-1-ylacetyl)azetidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[3-(pyrrolidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[3-(piperidin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(4-methylpiperazin-1-yl)acetyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-cyclopropylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-cyclopentylethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-3-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3,3-dimethylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclohexylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(3-methylbutyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopentylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(tetrahydrofuran-2-ylmethyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-methylpropyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(butylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(cyclopropylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(phenylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(4-fluorophenyl)sulfonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(ethylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(propan-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(benzylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(propylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(thiophen-2-ylsulfonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(2S)-2-methylbutanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(4,4-difluorocyclohexyl)carbonyl]azetidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(5-oxo-D-prolyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2,2-dimethylpropanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-methylpentanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(2-ethylbutanoyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(1H-pyrrol-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(1,2-oxazol-5-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(pyridin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(pyridazin-3-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(pyrazin-2-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(pyrimidin-4-ylcarbonyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[(5-methylpyrazin-2-yl)carbonyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[3-(piperidin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[1-(morpholin-4-ylacetyl)piperidin-4-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({1-[3-(4-methylpiperazin-1-yl)propanoyl]piperidin-4-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; benzyl trans-3-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]cyclobutanecarboxylate; N-[4-(4-{[(4-methylpiperazin-1-yl)acetyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydro-2H-pyran-4-ylacetyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[4-(benzoylamino)cyclohex-1-en-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(1-methylpiperidin-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(3R)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(3S)-tetrahydrofuran-3-ylcarbonyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(4-{[(2S)-2-methylbutanoyl]amino}cyclohex-1-en-1-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{3-[(3-methylbutanoyl)amino]oxetan-3-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; tert-butyl 4-({4-[(1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-ylcarbonyl)amino]phenyl}sulfonyl)piperidine-1-carboxylate; N-{4-[4-(propylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(2-methoxyethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(cyclopentylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(1,4-dioxan-2-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[4-(cyclopentylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[4-(tetrahydro-2H-pyran-4-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[4-(morpholin-4-ylcarbonyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[4-(cyclopropylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]piperidin-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[4-(butan-2-ylcarbamoyl)piperidin-1-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{(4R)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{(4S)-4-[(2-methylpropanoyl)amino]cyclohex-1-en-1-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-benzoylazetidin-3-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[trans-3-(benzylcarbamoyl)cyclobutyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{trans-3-[(2-phenylethyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{trans-3-[(3-phenylpropyl)carbamoyl]cyclobutyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methyl-1,3-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(furan-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2E)-3-(furan-2-yl)prop-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1,3-oxazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3,3,3-trifluoropropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,5-dimethyl-1H-pyrazol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(4-methoxycyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2,2-difluorocyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1H-pyrazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tert-butoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[3-(1H-1,2,4-triazol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3-ethoxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3-hydroxy-3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[3-(1H-pyrrol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methylpropoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1-methylprolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-hydroxycyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-{[1-(methoxymethyl)cyclopropyl]carbonyl}-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(methylsulfonyl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopropylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2E)-4-methylpent-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-methoxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopent-1-en-1-ylcarbonyl)-1,2,36-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(thiophen-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclohexylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-propanoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2,2-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2,2-dimethylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(4-methylhexanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2,2-dimethylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclobutylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(piperidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[2-(pyrrolidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,3-dimethyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(cis-4-{[(2-methoxyethoxy)acetyl]amino}cyclohex)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(trans-4-{[(2-methoxyethoxy)acetyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(cis-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(trans-4-{[(2S)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(cis-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(trans-4-{[(2R)-tetrahydrofuran-2-ylcarbonyl]amino}cyclohexyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(6-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3R)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3R)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({(3R)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({(3R)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3R)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3S)-1-(3-methylbutanoyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3S)-1-(cyclobutylcarbonyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({(3S)-1-[(2R)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({(3S)-1-[(2S)-tetrahydrofuran-2-ylcarbonyl]pyrrolidin-3-yl}oxy)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3S)-1-(cyclopropylacetyl)pyrrolidin-3-yl]oxy}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(6-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}pyridazin-3-yl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{6-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{6-[(cyclopentylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{6-[(tetrahydrofuran-3-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{6-[(bicyclo[2.2.1]hept-2-ylmethyl)carbamoyl]pyridazin-3-yl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{trans-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{cis-4-[(2-methylpropanoyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{cis-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{trans-4-[(cyclohexylcarbonyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{trans-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{cis-4-[(cyclopropylacetyl)amino]cyclohexyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; or a pharmaceutically acceptable salt thereof.
 8. The compound of claim 1, selected from the group consisting of: N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; and pharmaceutically acceptable salts thereof.
 9. The compound of claim 1, selected from the group consisting of: N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; and or a pharmaceutically acceptable salt thereof.
 10. The compound of claim 2, selected from the group consisting of: N-{4-[(3,5-dimethoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-chlorobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-phenylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydrofuran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-methylbutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(1S)-2-hydroxy-1-phenylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(1 S)-2-hydroxy-1-pyridin-2-ylethyl]amino}carbonyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3-methylbutyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(tetrahydrofuran-3-ylmethyl)amino]carbonyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(propylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2R)-tetrahydrofuran-2-ylmethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2S)-1-hydroxy-4-methylpentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1 S)-2-hydroxy-1-phenylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydro-2H-pyran-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1 S)-2-hydroxy-1-(pyridin-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-hydroxybutyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-1-hydroxy-3-methylbutan-2-yl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-hydroxy-2-methylpropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2R)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(2S)-2-hydroxypropyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(2-oxopyrrolidin-1-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3S)-tetrahydrofuran-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-isopropoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(isobutylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(butylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-methoxyethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(cyclopentylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-thienylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-isopropoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-isobutoxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyridin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyrimidin-4-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[2-(pyridin-3-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3-methyloxetan-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1,1-dioxidotetrahydrothiophen-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(pyrrolidin-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(3S)-pyrrolidin-3-ylmethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1-methylpyrrolidin-3-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1-methylpiperidin-4-yl)methyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(3R)-1-isobutyrylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[(3R)-1-benzoylpyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[1-(tetrahydrofuran-3-ylcarbonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[1-(methylsulfonyl)pyrrolidin-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[1-(morpholin-4-yl)cyclopentyl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1S)-1-(4-fluorophenyl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1 S)-2-hydroxy-1-(4-methoxyphenyl)ethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-({[3-(hydroxymethyl)oxetan-3-yl]methyl}carbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[(1S)-1-(1,3-benzodioxol-5-yl)-2-hydroxyethyl]carbamoyl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(1-oxa-8-azaspiro[4.5]dec-2-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-oxa-8-azaspiro[4.5]dec-3-ylcarbamoyl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[(2-oxa-9-azaspiro[5.5]undec-3-ylmethyl)carbamoyl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{[3-(5-methyl-1H-pyrazol-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(4-chloro-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(3,5-dimethyl-1H-pyrazol-1-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-methyl-2-(morpholin-4-yl)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[3-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-carbamoylbenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-amino-1-oxohexan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(3,4-dimethoxyphenyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; Nalpha-{4-[(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-ylcarbonyl)amino]benzoyl}-L-phenylalaninamide; N-(4-{[(2R)-1-amino-4-methyl-1-oxopentan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-tert-butoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(2,6-dimethylmorpholin-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-methoxybenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-methyl-2-(morpholin-4-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(3S)-1-methyl-2-oxoazepan-3-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(4-methylpiperazin-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[4-(morpholin-4-yl)benzyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[3-(piperidin-1-yl)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-(4,5,6,7-tetrahydro-1H-indazol-5-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-methoxy-2,2-dimethylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3,3-dimethylbutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(furan-2-yl)propan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(3-methyl-1,2-oxazol-5-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2R)-1-cyanobutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1-methyl-1H-pyrazol-3-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[4-(dimethylamino)butyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(1,3-thiazol-2-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(1-methyl-1H-pyrazol-4-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3S)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-methoxybutan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-ethoxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(6-methoxypyridin-3-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2S)-butan-2-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-cyanocyclopropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(5-methyl-1H-pyrazol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(4-methyl-1,3-thiazol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-hydroxypropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydrofuran-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1R)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[1-(1-methylcyclopropyl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(thiophen-2-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1S)-1-cyclopropylethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(4-methoxybutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(tetrahydro-2H-pyran-3-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2S)-1-methoxypropan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3,3-dimethyl-2-oxobutyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(1-methyl-1H-pyrrol-2-yl)methyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(propan-2-yloxy)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[3-(dimethylamino)propyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-(tetrahydro-2H-pyran-3-ylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[2-(1H-pyrrol-1-yl)ethyl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-methoxypropan-2-yl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3-aminobenzyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-(4-{[(2R)-3-methylbutan-2-yl]carbamoyl}phenyl)-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(tetrahydro-2H-pyran-3-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-hydroxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-[4-(butylcarbamoyl)phenyl]-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(1-cyanoethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(3R)-tetrahydrofuran-3-ylcarbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(cyclopentylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(2-methoxy-2-methylpropyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(cyclopropylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; N-{4-[(pyridin-4-ylmethyl)carbamoyl]phenyl}-5,7-dihydro-6H-pyrrolo[3,4-b]pyridine-6-carboxamide; or a pharmaceutically acceptable salt thereof.
 11. The compound of claim 3, selected from the group consisting of: N-[4-(1-butyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutyryl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-benzoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methoxyethoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-isobutyrylpiperidin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1,4-dioxan-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(morpholin-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1,4-dioxan-2-ylcarbonyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylpyrrolidin-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(morpholin-4-ylacetyl)piperidin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylpiperidin-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-4-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(N,N-dimethylglycyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(4-methylpiperazin-1-yl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopentylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydro-2H-pyran-2-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(pyrrolidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(pyrazin-2-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3S)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(3R)-tetrahydrofuran-3-ylcarbonyl]piperidin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methyl-1,3-oxazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(furan-3-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2E)-3-(furan-2-yl)prop-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1,3-oxazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3,3,3-trifluoropropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,5-dimethyl-1H-pyrazol-3-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(4-methoxycyclohexyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2,3-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2,2-difluorocyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1H-pyrazol-5-ylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tert-butoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[3-(1H-1,2,4-triazol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3-ethoxypropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(3-hydroxy-3-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[3-(1H-pyrrol-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methylpropoxy)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(1-methylprolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-hydroxycyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopropylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopentylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-{[1-(methoxymethyl)cyclopropyl]carbonyl}-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(methylsulfonyl)acetyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopropylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-ethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(5-oxo-L-prolyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2E)-4-methylpent-2-enoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-methoxy-2-methylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopent-1-en-1-ylcarbonyl)-1,2,36-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(thiophen-3-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclohexylcarbonyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-[4-(1-propanoyl-1,2,3,6-tetrahydropyridin-4-yl)phenyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2,2-dimethylbutanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(methoxyacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2,2-dimethylpropanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(4-methylhexanoyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2,2-dimethylcyclopropyl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,3-dimethyl-1H-pyrazol-5-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclobutylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(piperidin-1-ylacetyl)-1,2,3,6-tetrahydropyridin-4-yl]phenyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[2-(pyrrolidin-1-yl)propanoyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,3-dimethyl-1H-pyrazol-4-yl)carbonyl]-1,2,3,6-tetrahydropyridin-4-yl}phenyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; or a pharmaceutically acceptable salt thereof.
 12. The compound of claim 4, selected from the group consisting of: N-[4-(1-benzoylpiperidin-4-yl)butyl]-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-chlorobenzoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-2-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(1,1-dioxidotetrahydrothiophen-3-yl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclohexylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(4,4-difluorocyclohexyl)carbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(2-hydroxy-2-methylpropanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2R)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2S)-tetrahydrofuran-2-ylcarbonyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(2-methoxyethoxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(tetrahydrofuran-3-ylcarbonyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-(4-{1-[(propan-2-yloxy)acetyl]piperidin-4-yl}butyl)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(cyclopropylacetyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; N-{4-[1-(4,4,4-trifluorobutanoyl)piperidin-4-yl]butyl}-1,3-dihydro-2H-pyrrolo[3,4-c]pyridine-2-carboxamide; or a pharmaceutically acceptable salt thereof.
 13. A compound having Formula (IIc), or a pharmaceutically acceptable salt thereof

wherein X¹ and X³ are CH; and X² is N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂; R² is phenyl, thiophenyl, pyrazolyl, thiazolyl, pyridinyl, pyridazinyl, pyrazinyl, cycloalkyl, or cycloalkenyl; wherein each R² phenyl is substituted at the para position with one independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; wherein each R² phenyl is optionally additionally substituted with one F; wherein each R² heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl; R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I; R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R¹⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR⁶, OH, F, Cl, Br, or I; R¹⁵, at each occurrence, is independently selected alkyl; wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.
 14. The compound of claim 13, or a pharmaceutically acceptable salt thereof; wherein X¹ and X³ are CH; and X² is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH.
 15. A compound having Formula (IIIc), or a pharmaceutically acceptable salt thereof

wherein X¹ and X³ are CH; and X² is N; or X² and X³ are CH; and X¹ is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is CH; or X¹ is N; X² is CR¹; and X³ is N; R¹ is R³, OR³, SR³, S(O)R³, SO₂R³, C(O)R³, C(O)OR³, OC(O)R³, NHR³, N(R³)₂, C(O)NH₂, C(O)NHR³, C(O)N(R³)₂, NHC(O)R³, NR³C(O)R³, NHC(O)OR³, NR³C(O)OR³, SO₂NH₂, SO₂NHR³, SO₂N(R³)₂, NHSO₂R³, NR³SO₂R³, NHSO₂NHR³, NHSO₂N(R³)₂, NR³SO₂NHR³, NR³SO₂N(R³)₂, C(O)NHSO₂R³, NHSO₂NHR³, F, Cl, Br, I, CN, NH₂, NO₂, N₃, OH, C(O)H, CF₃, C(O)OH, or C(O)NH₂; R^(x) is R⁵, OR⁵, SR⁵, S(O)R⁵, SO₂R⁵, C(O)R⁵, CO(O)R⁵, OC(O)R⁵, OC(O)OR⁵, NH₂, NHR⁵, N(R⁵)₂, NHC(O)R⁵, NR⁵C(O)R⁵, NHS(O)₂R⁵, NR⁵S(O)₂R⁵, NHC(O)OR⁵, NR⁵C(O)OR⁵, NHC(O)NH₂, NHC(O)NHR⁵, NHC(O)N(R⁵)₂, NR⁵C(O)NHR⁵, NR⁵C(O)N(R⁵)₂, C(O)NH₂, C(O)NHR⁵, C(O)N(R⁵)₂, CHNOR⁵, C(O)NHOH, C(O)NHOR⁵, C(O)NHSO₂R⁵, C(O)NR⁵SO₂R⁵, SO₂NH₂, SO₂NHR⁵, SO₂N(R⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, Br or I; R³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, or heterocyclyl; wherein each R³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁶, OR⁶, SR⁶, S(O)R⁶, SO₂R⁶, C(O)R⁶, CO(O)R⁶, OC(O)R⁶, OC(O)OR⁶, NH₂, NHR⁶, N(R⁶)₂, NHC(O)R⁶, NR⁶C(O)R⁶, NHS(O)₂R⁶, NR⁶S(O)₂R⁶, NHC(O)OR⁶, NR⁶C(O)OR⁶, NHC(O)NH₂, NHC(O)NHR⁶, NHC(O)N(R⁶)₂, NR⁶C(O)NHR⁶, NR⁶C(O)N(R⁶)₂, C(O)NH₂, C(O)NHR⁶, C(O)N(R⁶)₂, C(O)NHOH, C(O)NHOR⁶, C(O)NHSO₂R⁶, C(O)NR⁶SO₂R⁶, SO₂NH₂, SO₂NHR⁶, SO₂N(R⁶)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁵, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁵ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R⁶, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁶ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, NHR¹⁰, N(R¹⁰)₂, C(O)R¹⁰, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHSO₂R¹⁰, NHC(O)OR¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, NHC(O)NH₂, NHC(O)NHR¹⁰, OH, (O), C(O)OH, N₃, CN, NH₂, CF₃, CF₂CF₃, F, Cl, Br or I; R⁹, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R⁹ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected alkoxy, OH, cycloalkyl, aryl, or heterocyclyl; R¹⁰, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein the cyclic moieties represented by R³, R⁵, R⁶, R⁹, and R¹⁰ are optionally substituted with one, two, three, four, five, or six independently selected R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³, NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³, NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R³)₂, C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³, C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, SCF₃, F, Cl, Br or I; R¹³, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, or cycloalkenyl; wherein each R¹³ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected R¹⁴, OR¹⁴, SR¹⁴, S(O)R¹⁴, SO₂R¹⁴, C(O)R¹⁴, OC(O)R¹⁴, OC(O)OR¹⁴, NH₂, NHR¹⁴, N(R¹⁴)₂, NHC(O)R¹⁴, NR¹⁴C(O)R¹⁴, NHS(O)₂R¹⁴, NR¹⁴S(O)₂R¹⁴, NHC(O)OR¹⁴, NR¹⁴C(O)OR¹⁴, NHC(O)NH₂, NHC(O)NHR¹⁴, NHC(O)N(R¹⁴)₂, NR¹⁴C(O)NHR¹⁴, NR¹⁴C(O)N(R⁴)₂, C(O)NH₂, C(O)NHR¹⁴, C(O)N(R¹⁴)₂, C(O)NHOH, C(O)NHOR¹⁴, C(O)NHSO₂R¹⁴, C(O)NR¹⁴SO₂R¹⁴, SO₂NH₂, SO₂NHR¹⁴, SO₂N(R¹⁴)₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹³ aryl, tetrahydrofuranyl, pyridazinyl, pyrazinyl, pyrimidinyl, pyridinyl, thieno[3,2-c]pyridinyl, furo[3,2-c]pyridinyl, pyrrolidin-2-onyl, 1,1-dioxidotetrahydrothien-3-yl, 1,1-dioxidotetrahydro-2H-thiopyran-3-yl, dioxanyl, tetrahydropyranyl, piperidinyl, pyrimidinyl, oxazolyl, pyrazolyl, thiazolyl, pyrrolidinyl, pyrrolyl, thienyl, furanyl, morpholinyl, isooxazolyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁵, OR¹⁵, SR¹⁵, S(O)R¹⁵, SO₂R¹⁵, C(O)R¹⁵, CO(O)R¹⁵, OC(O)R¹⁵, OC(O)OR¹⁵, NH₂, NHR¹⁵, N(R¹⁵)₂, NHC(O)R¹⁵, NR¹⁵C(O)R¹⁵, NHS(O)₂R¹⁵, NR¹⁵S(O)₂R¹⁵, NHC(O)OR¹⁵, NR¹⁵C(O)OR¹⁵, NHC(O)NH₂, NHC(O)NHR¹⁵, NHC(O)N(R¹⁵)₂, NR¹⁵C(O)NHR¹⁵, NR¹⁵C(O)N(R¹⁵)₂, C(O)NH₂, C(O)NHR¹⁵, C(O)N(R¹⁵)₂, C(O)NHOH, C(O)NHOR¹⁵, C(O)NHSO₂R¹⁵, C(O)NR¹⁵SO₂R¹⁵, SO₂NH₂, SO₂NHR¹⁵, SO₂N(R¹⁵)₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; R¹⁴, at each occurrence, is independently selected alkyl, alkenyl, alkynyl, aryl, heterocyclyl, cycloalkyl, or cycloalkenyl; wherein each R¹⁴ alkyl, alkenyl, and alkynyl is optionally substituted with one, two, three or four independently selected heterocyclyl, alkoxy, NH₂, SO₂NH₂, C(O)H, C(O)OH, OH, (O), CN, N₃, NO₂, CF₃, CF₂CF₃, OCF₃, OCF₂CF₃, F, Cl, Br or I; wherein each R¹⁴ aryl, heterocyclyl, cycloalkyl, and cycloalkenyl is optionally substituted with one, two, three or four independently selected R¹⁶, OR⁶, OH, F, Cl, Br, or I; R¹⁵, at each occurrence, is independently selected alkyl, wherein the R¹⁵ alkyl is optionally substituted with one, two, three or four alkoxy; and R¹⁶, at each occurrence, is independently selected alkyl, wherein the R¹⁶ alkyl is optionally substituted with one, two, three or four alkoxy; with the proviso that when R¹³ is piperidinyl, it is substituted piperidinyl.
 16. The compound of claim 15, or a pharmaceutically acceptable salt thereof; wherein X¹ and X³ are CH; and X² is N; or X¹ is CH; X² is N; and X³ is CR¹; or X¹ is CR¹; X² is N; and X³ is CH.
 17. The compound of claim 16, or a pharmaceutically acceptable salt thereof; wherein R^(x) is R⁵; and R⁵ is heterocyclyl.
 18. A composition comprising an excipient and a therapeutically effective amount of a compound of claim 1, or a pharmaceutically acceptable salt thereof. 